Antitumor activity
Several new nitrobenzimidazoles have been reported to possess cytotoxic activity against breast cancer. In the reported research it was also found out that the compounds like thiadiazole, tetrazole, triazines and imidazolesalso possess the activity .[50]

Anti prozoal Activity
Benzimidazole derivatives reported are 5, 6 dinitro and thioalkyl or thioaryl substituted compounds .These active compounds reported to possess activity against Stenotrophomonas malthophilia. These compounds have activity related to metronidazole against gram positive and gram negative bacteria. Substituted 2- trifluorobenzimidazoles have been reported.[56, 57] Earlier it have reported anti-giardial activity.[58, 59] One of another research involves the synthesis of series of 2-(trifluoromethyl)- 1H- Benzimidazole derivatives by using Phillips cyclocondensation of a substituted 1,2-phenylenediamine and trifluoroacetic acid.

The compounds were evaluated in vitro against various protozoan parasites naming Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis and Leishmania mexicana,and they showed nanomolar activities against some of the above mentioned protozoa. The compounds were also tested in vitro and in vivo against the nematode Trichinella spiralis.[60]

Antiparasitic Activity
2-(Trifluoromethyl)-1Hbenzimidazole derivatives showed the most desirable in vitro antiparasitic profile against Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis and Trichinella spiralisThe anthelmintic drugs derived from benzimidazole 2-carbamates, such as albendazole (ABZ) and mebendazole (MBZ), are used mainly to treat endoparasitic diseases in domestic animals and humans. These types of compounds are characterized by a high therapeutic index and low toxicity; however, they find little use in tissue-dwelling parasites mainly due to poor solubility and absorption problems.

Antiulcer activity
Substituted Benzimidazoles are potent inhibitors of Parietal cell proton pump, the H+/K+ ATPase, the substituted benzimidazoles are capable of blocking gastric acid secretion in response to some stimuli. For the activity sulfoxide group, methylene group with hetercycles is important for activity.[43]

Anti-inflammatory activity
Benzimidazole is one of the most promising heteroaryl moiety that yielded many successful drugs like omeprazole and mebendazole. Benzimidazole moiety with carboxylic acid substitution at 2 position, fulfills the minimum and desirable structural requirements that are common in most of the marketed anti-inflammatory drugs and so some benzimidazole-2-carboxylic acid Derivatives were synthesized. They were tested for acute anti-inflammatory activity against carrageenan induced rat paw edema model. The test compounds were found to be safe 2000 mg/kg, p.o. doses and exhibited good anti-inflammatory activity at 100 mg/kg p.o. and higher doses. The anti-inflammatory effect against carrageenan edema suggests inhibition of prostaglandin synthesis as their probable mechanism of action.

Non steroidal anti-inflammatory drugs (NSAIDs) are one of the most widely used drug category against inflammation, mild to moderate pain, and fever. Specific uses also include the treatment of headaches, arthritis, sports injuries, and menstrual cramps. Their use is mainly restricted by their well known and serious adverse gastrointestinal side effects[66-70] such as gastroduodenal erosions and ulceration. Therefore, search for better and safer anti-inflammatory agents is always going on at a rapid pace.

A series of 2- methylaminobenzimidazole derivatives were synthesized and reported [51] by the reaction of 2-(chloromethyl)-1H-benzimidazole derivatives with primary aromatic amines The new synthesized compounds were screened for analgesic and anti-inflammatory activities by the author on acetic acid induced writhing in mice and carrageenan induced paw oedema in rats. Some Compounds showed a potent analgesic (89% at 100 mg/kg b.w) and anti-inflammatory (100% at 100 mg/kg b.w) activities compared with standard drug Nimesulide (100% at 50 mg/kg b.w) respectively. Another research was carried out indicating that benzimidazole on combination with iodole Skelton give potent anti inflammatory action similar to indomethacin.[52] A series of benzamides has been synthesized with N – acridin -9-yl substituent.[53]

Anti-Oxidant activity
Some compounds possessing dihydrochlorides have also been reported possessing antioxidant activity, these salts also possess mild platelet and erythrocyte antiaggregant activity.[54] In another approach it was found out that using trimethyl group with benzimidazole also adds antioxidative property by 5-lipoxygenase inhibitory action.[55]

HIV Inhibtors:-
Tetrahydro-imidazo[1,4]-benzodiazepin-2(1H)one(TIBO) is a noncompetitive non nucleotide antiretroviraldrug with a specific allosteric binding site of HIV-1 RT. TIBO derivatives have proved to be potent, highly selective and specific inhibitors of HIV-1 replication in vitro. The reverse transcriptase (RT) of HIV-1, but not HIV-2, is inhibited by the TIBO compounds. Several compounds other than TIBO have recently been reported to specifically inhibit HIV-1 replication. In a research it was investigated that some novel benzimidazole derivatives, bearing analogy to TIBO, have been synthesized, and were evaluated for inhibition of HIV-1 infectivity. The most active and selective compounds are a series of N-alkoxy- 2-alkyl-benzimidazoles, several having EC50 < 10Μm (one sub-micromolar at 600nM), and selectivity ratios of 10–167. The selective benzimidazoles, show modest RT inhibition.[33]

Benzimidazole is an important heterocyclic moiety for the discovery of new drugs. This has been noticed so far, that modifications on benzimidazole moiety displayed valuable

biological activities. It will be interesting to observe that these modifications can be utilized as potent therapeutic agents in future. The knowledge gained by various researches has suggested that  substituted benzimidazoles and heterocycles,  which are the structural isosteres of nucleotides allow them to interact easily with the biopolymers, possess pharmacological activity with lower toxicities. Since now, researchers have been attracted toward designing more potent Benzimidazole  derivatives having wide diverse of biological  activity

1. Barker HA, Smyth RD, Weissbach H,Toohey JI, Ladd JN and Volcani BE. Isolation and properties of crystalline cobamide coenzymes containing Benzimidazole or 5,6- Dimethylbenzimidazole. Journal of Biological Chemistry. 1960;235(2):480- 488.
2. Patil A, Ganguly S and Surana S. A systematic review of benzimidazole derivatives as an antiulcer agent. Rasayan J Chem. 2008;1(3):447-460
3. Kubo K, Oda K, Kaneko T, Satoh H and Nohara A. Synthesis of 2-(4- Fluoroalkoxy-2-pyridyl) methyl] sulfinyl]-1H-benzimidazoles as Antiulcer Agents. Chem Pharm Bull. 1990;38(10):2853-2858.
4. Uchida M, Chihiro M, Morita S, Yamashita H, Yamasaki K, Kanbe T, Yabuuchi Y and Nakagawz K. Synthesis and Antiulcer Activity of 4- Substituted 8-[(2 Benzimidazolyl) sulfinylmethyl]-1, 2, 3, 4-tetrahydroquinolines and Related Compounds. Chem Pharm Bull. 1990;38(6):1575-1586.
5. Grassi A, Ippen J, Bruno M, Thomas G and Bay P. A thiazolylamino benzimidazole derivative with gastroprotective properties in the rat. Eur J Pharmacol. 1991;195(2):251-9.
6. Ozkay Y, Tunali Y, Karaca H. and Isikdag I. Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazones moiety. European Journal of Medicinal Chemistry. 2010;45(8):3293-3298.
7. Yun H, Baogen W, Yang J, Robinson D, Risen L, Ranken R, Blyn L, Eric SS. and Swayze E. 2-Piperidin-4-ylbenzimidazoles with Broad Spectrum antibacterial activities. Bioorg Med Chem Lett. 2003;13:3253-3256.
8. Metwally KA, Abdel-Aziz LM, Lashine el-SM, Husseiny MI and Badawy RH. Hydrazones of 2-aryl- -4- carboxylic acid hydrazides: synthesis and preliminary evaluation as antimicrobial agents. Bioorg Med Chem. 2006;14(24): 8675-82.
9. Spasov A, Yozhitsa L, Bugaeva I and Anisimova VA. Benzimidazole derivatives: Spectrum of pharmacological activity and toxicological properties.Pharmaceutical Chemistry Journal. 33;5:232-243.
10. Arjmand F, Mohani B and Ahmad S. Synthesis, antibacterial, antifungal activity and interaction of CT-DNA with a new benzimidazole derived Cu (II) complex. Eur J Med Chem. 2005;40(11):1103-1110.
11. Preston PN. Benzimidazoles and Congeneric Tricyclic Compounds Part 2.Wiley Interscience New York, 1980:531.
12. Foks H, Ksepko DP, Kuzmierkiewicz W, Zwolska Z, Augustynowicz EK, and Janowiec M. Synthesis and tuberculostatic activity of new benzimidazole derivatives. Chem Het Comp. 2006;42:611-614.
13. Ansari KF and Lal C. Synthesis, physicochemical properties and antimicrobial activity of some new Benzimidazole derivatives. European Journal of Medicinal Chemistry. 2009;44:4028–4033.
14. Göker H, Kus C, Boykin D.W, Yildiz S and Altanlar N. Synthesis of some new 2-substitutedphenyl-1Hbenzimidazole- 5-carbonitriles and their potent activity against Candida species. Bioorg Med Chem. 2002;10: 2589-2596.
15. Klimesová V, Kocí J, Pour M, Stachel J, Waisser K and Kaustová J. Synthesis and preliminary evaluation of benzimidazole derivatives as antimicrobial agents. Eur J Med Chem.2002;37:409 - 418.
16. Khalafi-Nezhad A, Soltani Rad MN, Mohabatkar H, Asrari Z and Hemmateenejad B. Design, synthesis, antibacterial and QSAR studies of benzimidazole and imidazole chloroaryloxyalkyl derivatives. Bioorg Med Chem. 2005;13:1931-1938.
17. Ayhan-Kilcigil G and Altanlar N. Synthesis and antimicrobial activities of some new benzimidazole derivatives. Farmaco. 2003;58:1345- 1350.
18. Pawar NS, Dalal DS, Shimpi SR and Mahulikar PP. Studies of antimicrobial activity of N-alkyl and N-acyl 2-(4- thiazolyl)-1H-benzimidazoles. Eur J Pharm Sci. 2004;21:115-118.
19. Boiani M and Gonzalez M. Imidazole and Benzimidazole Derivatives as Chemotherapeutic Agents. Mini Rev Med Chem. 2005;5:409-424.
20. Desai KG and Desai KR. Green route for the heterocyclization of 2-mercaptobenzimidazole into betalactum segment derivatives containingn-CONH- bridge with Benzimidazole. Screening in vitro antimicrobial activity with various microorganisms. Bioorg Med Chem. 2006;14:8271-8279.
21. Mohammad BG, Hussien MA, Abdel- Alim AA and Hashem M. Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4 triazolobenzimidazole Derivatives. Arch Pharm Res. 2006;29:26-33.
22. Guven OO, Erdogan T, Goker H and Y?ld?z S. Synthesis and antimicrobial activity of some novel phenyl and benzimidazole substituted benzyl ethers. Bioorg Med Chem Lett. 2007;17: Tuncbilek M, Kiper T and Altanlar N.
23. Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA. Eur J Med Chem. 2009;44:1024-1033.
24. Sharma D, Narasimhan B, Kumar P and Jalbout A. Synthesis and QSAR evaluation of 2-(substituted phenyl)- 1H-benzimidazoles and [2- (substituted phenyl)-benzimidazol-1- yl]-pyridin-3-yl-methanones. Eur J Med Chem. 2009;44:1119-1127.
25. Chornous VA, Bratenko MK, Vovk MV and Sidorchuk II. Synthesis and Antimicrobial Activity of Pyrazole-4- carboxylic Acid Hydrazides and N-(4- Pyrazoyl)hydrazones of Aromatic and Heteroaromatic Aldehydes. Pharmaceutical Chemistry Journal. 2001;35(4):203-205.
26. Rollas S, Gulerman N and Erdeniz H. Synthesis and antimicrobial activity of some new hydrazones of 4- fluorobenzoic acid hydrazide and 3- acetyl-2,5-disubstituted-1,3,4- oxadiazolines. Farmaco. 2002;57:171-174.
27. Papakonstantinou GS, Pouli N, Marakos P and Chytyroglou LA. Synthesis antimicrobial and antifungal activity of some new 3-substituted derivatives of 4-(2, 4-dichlorophenyl)- 5-adamantyl-1H-1,2,4-triazole. Farmaco. 2002;57:973-977.
28. Vicini P, Zani F, Cozzini P and Doytchinova I. Hydrazones of 1, 2-benzisothiazole hydrazides: synthesis, antimicrobial activity and QSAR investigations. Eur J Med Chem.2002;37:553-564.
29. Loncle C, Brunel JM, Dherbomez M, and Letourneux Y. Synthesis and antifungal activity of cholesterolhydrazone derivatives. Eur J Med Chem. 2004;39:1067-1071.
30. Salg?n-Goksen U, Gokhan-Kelekci U, Goktas O, Koysal Y, K?l?c E, Isik S, Aktay G and Ozalp M. 1- Acylthiosemicarbazides, 1, 2, 4- triazole-5(4H)-thiones, 1, 3, 4- thiadiazoles and hydrazones containing 5-methyl-2- benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities. Bioorg Med Chem. 2007;15:5738-5751.
31. Masunari A and Tavares LC. A new class of nifuroxazide analogues: synthesis of 5-nitrothiophene derivatives with antimicrobial activity against multidrug-resistant Staphylococcus aureus. Bioorg Med Chem. 2007;15:4229-4236.
32. Göker H, Ozden S, Yildiz S and Boykin DW. Synthesis and potent antibacterial activity against MRSA of some novel 1,2-Disubstituted-1HBenzimidazole- N-alkylated-5- carboxamidine. Eur J Med Chem. 2005;40:1062 -1069.
33. Gardiner JM, Loyns CR, Burke A, Khan A and Mahmood N. Synthesis and HIV-1 inhibition of novel benzimidazole derivatives, Bioorganic & Medicinal Chemistry Letters. 1995;5(12):1251-1254.
34. Hernández-Luis F, Hernández- Campos A, Castillo R, Navarrete- Vázquez G, Soria-Arteche O, Hernández-Hernández M and Yépez- Mulia L. European Journal of Medicinal Chemistry. 2010;45(7):3135.
35. Cook GC. Use of benzimidazole chemotherapy in human helminthiases: indication and efficacy, Parasitol. Today. 1990;(6):133–136.
36. Eggers, Hans J, Tamm and Igor. Inhibition of enterovirus ribonucleic acid synthesis by 2-(alphahydroxybenzyl) benzimidazole. Nature. 1963;197:1327.
37. Sullivan DG, Pantic D and Wallis AK. New 1, 2-disubstituted benzimidazoles with high inhibiting effects on poliovirus replication. Experentia. 1967;23:704.
38. Tewari AK and Mishra A. Synthesisand antiviral activities of Nsubstituted -2-substituted - benzimidazole derivatives. Ind J Chem. 2006;45(B):489-493.
39. Starcevic K, Kralj M, Ester K, Sabol I, Grce M, Pavelic K and Karminski- Zamola G. Synthesis, antiviral and antitumor activity of 2-substituted-5- amidino benzimidazoles. Bioorg Med Chem. 2007;15(13):4419-4426.
40. Fei Xue, Xianjin Luo, Chenghao Ye, Weidong Ye and Wang Y. Inhibitory derivatives against enteroviruses. Bioorganic Medicinal Chemistry. 2011;19(8):2641-2649.
41. Shah DI, Sharma M, Bansal Y, Bansal G and Singh M. Angiotensin II--AT1 receptor antagonists: design, synthesis and evaluation of substituted carboxamido benzimidazole derivatives. Eur J Med Chem. 2007;20:1-5.
42. Jat RK, Jat JL and Pathak DP. Synthesis of benzimidazole derivatives: As Anti-hypertensive agents. E- Journal of Chem. 2006;3:278.
43. Dubey PK, Naidu A, Reddy PV, Kumar NDM, and Vineel BG. Studies on synthesis of unsymmetrical 2,21- bisbenzimidazole sulphides of pharmacological interest. Ind J Chem. 2008;47:1443.
44. Rajanarendar E, Ramu K, Reddy ASR and Shaik FP. Synthesis and in vitro study of novel isoxazolyl benzoimidazolyl benzamides, acrylamides and propionamides as antimicrobial agents. Ind J Chem. 2008;47:1284.
45. Jubie S, Rajeshkumar R, Yella reddy B, Siddhartha G, Sandeep M, Surendrareddy K, Dushyatha HS And Elango K. Microwave assisted synthesis of some novel Benzimidazole submitted fluoroquinolones and their antimicrobial evaluation. J Pharm Sci and Res. 2010;2(2):69-76.
46. Klimesova V, Koc? J, Waisser K and Kaustova J. New Benzimidazole derivatives as antimycobacterial agents. IL Farmaco. 2002;57:259–265.
47. Göker H, Alp M and Yildiz S. Synthesis and potent Antimicrobial activity of some novel N-(alkyl)-2- Phenyl-1H-benzimidazole-5- carboxamidines. Molecules. 2005;10:1377-1386.
48. Ansari KF and Lal C. Synthesis and evaluation of some new Benzimidazole derivatives as potent antimicrobial agents. European Journal of Medicinal Chemistry. 2009;44:2294–2299.
49. Nawrocka W, Sztuba B, Kowalska M W, Liszkiewicz H, Wietrzyk J, Nasulewicz A, Pe?czynska M and Opolski A. Synthesis and antiproliferative activity in vitro of 2-aminobenzimidazole derivatives. IL Farmaco. 2004;59:83–91.
50. Ramla MM, Omar MA, EL Khamry AM and EL Diwani HI. Synthesis and antitumor activity of 1-substituted-2- methyl-5-nitrobenzimidazoles. Bioorg Med Chem. 2006;14:7324-7332.
51. Kavitha CS, Achar, Kallappa M. Hosamani, Harisha R. Seetharamareddy. In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives. European Journal of Medicinal Chemistry. 2010;45:2048– 2054.
52. Dubey PK, Babu B, Narayana MV. Synthesis of 2-indolylbenzimidazoles using Fischer’s indole method. Indian Journal of chemistry. 2007;46:823-828.
53. Sondhi SM, Singh N, Kumar A, Lozach O and Meijer L. Synthesis, anti-inflammatory, analgesic and kinase (CDK-1, CDK-5 and GSK-3) inhibition activity evaluation of Benzimidazole/benzoxazole derivatives and some Schiff's bases. Bioorg Med Chem. 2006;14:3758-3765.
54. Anisimova VA, Spasov AA, Kosolapov VA, Tolpygin IE, Kucheryavenko AF, Sysoeva VA, Tibirkova EV and Eltsova LV. Synthesis and pharmacological activity of 3-(2,2,2-trichloro-1- hydroxyethyl) imidazo[1,2- a]Benzimidazole dihydrochlorides. Pharmaceutical Chemistry Journal.2009;43:491-494.
55. Nikano H and Inoue T. Synthesis of Benzimidazole derivatives as antiallergic agents with 5- lipoxygenase inhibiting action. Chem Pharm Bull. 1999;47(11):1573.
56. Kazimierczuk Z, Upcroft JA, Upcroft P, Gorska A, Starosciak B and Agnieszka L. Acta Biochimica polonica. 2002;49:185- 195.
57. Navarrete-Vázquez G, Cedillo R, Hernández-Campos A, Yepez L Hernández-Luis FJ, Valdéz R, Morales R, Cortés M, and Castillo R. Synthesis and antiparasitic activity of 2-(trifluoromethyl) benzimidazole derivatives. Bioorg Med Chem Lett. 2001;11:187–190.
58. Xiao L, Saeed K and Herd RP. Efficacy of albendazole and fenbendazole against Giardia Infection in cattle Vet. Parasitol. 1996;61:165- 170.
59. Katiyar SK, Gordon VR, McLaughlin GL and Edlind TD. Antiprotozoal activities of benzimidazoles and correlations with beta-tubulin sequence. Antimicrob Agents Chemother. 1994;38:2086- 2090.
60. Hernández-Luis F, Hernández- Campos A, Castillo R, Navarrete-Vázquez G, Soria-Arteche O, Hernandez Hernandez M and Yépez- Mulia L. Synthesis and biological activity of 2-(trifluoromethyl)-1Hbenzimidazole derivatives against some protozoa and Trichinella spiralis. European Journal of Medicinal Chemistry. 2010;45(7):3135- 3141.
61. Raymond A. Ng, Guan J, Alford VC Jr, lanter JC, Allan GF, Sbriscia T, Linton O, Lundeen SG and Sui Z. Synthesis and Sar of potent and selective androgen receptor antagonists: 5, 6 dichloro Benzimidazole derivatives. Bioorg Med Chem Lett. 2007;17:784-
62. Negro-Vilar A. Selective Androgen Receptor Modulators (SARMs) A Novel Approach to Androgen Therapy for the new millennium. J Clin Endocrinol Metab. 1999;84:3459 - 3462.
63. Demirayaka S, Kayagilb I and Yurttasc L. Microwave supported synthesis of some novel 1, 3- Diarylpyrazino [1, 2-a] benzimidazole derivatives and investigation of their anticancer activities. European Journal of Medicinal Chemistry. 2011;46(1):411-416.
64. Gowda NR, Kavitha CV, Chiruvella KK, Joy O, Rangappa KS and Raghavan SC. Synthesis and biological evaluation of novel 1-(4- methoxyphenethyl) 1Hbenzimidazole- 5-carboxylic acid derivatives and their precursors as antileukemic agents. Bioorg Med Chem Lett. 2009;19(16):4594-600.
65. Singh J, Grover P and Pathak DP. Synthesis, anticonvulsant activity and comparative QSAR study of some novel 1, 2, 5-trisubstituted benzimidazole derivatives. Acta Pharmaceutica Sciencia. 2010;52:511-522.
66.Chan FK. Primer: managing NSAID-induced ulcer complications—balancing gastrointestinal and cardiovascular risks. Nature clinical practice. 2006 Oct;3(10):563-732.
67.Whittle BJ. Mechanisms underlying intestinal injury induced by anti-inflammatory COX inhibitors. Eur J Pharmacol. 2004 Oct1;500(13):427-39.
68. Cryer B. The role of cyclooxygenase selective inhibitors in the gastrointestinal tract. Current gastroenterology reports. 2003 Dec;5(6):453-8.
69. Bjorkman DJ. Nonsteroidal anti-inflammatory drug-induced gastrointestinal injury. The American journal of medicine. 1996 Jul 31;101(1A):25S-32S.
70. Kimmey MB. NSAID, ulcers, and prostaglandins. The Journal of rheumatology. 1992 Nov;36:68-73.
71. Richy F, Bruyere O, Ethgen O, Rabenda V, Bouvenot G, Audran M, et al. Time dependent risk of gastrointestinal complications induced by non-steroidal anti-inflammatory drug use: a consensus statement using a meta-analytic approach. Annals of the rheumatic diseases. 2004 Jul;63(7):759-66.
72. Scherrer RA. Antiinflammatory drugs : Chemistry and Pharmacology In: Scherrer RA, Woodhouse MW, editors. London: Academic press; 1974. p. 119-22.
73. Nicholson RM, Murphy JR, Dearden JR. Hypothetical receptor model for antiinflammatory agents. Journal of Pharmacy and Pharmacology. 1982;34(Suppl):106P.
74. Gund P, Jensen NP. Nonsteroidal antiinflammatory and anti-arthritic drugs. In: Blankley J, editor. Quantitative structure activity relationships of drugs. New York. : Academic press; 1983. p. 285-326.
75. Borne RF. Nonsteroidal antiinflammatory drugs. In: Foye WO, editor. Principles of medicinal chemistry. 5th ed. Philadelphia: Lea & Fabiger,; 1995. p. 535-79.
76. Preston PN. Benzimidazoles. In: Preston PN, editor. Chemistry of heterocyclic compounds: Benzimidazoles. New York: Wiley-Intrescience; 1980. p. 1-281.
77. Cain CK, Reoszkowasky AP. Benzoxazoles, Benzothiazoles and Benzimidazoles. In: Arians EJ, editor. Medicinal Chemistry: Series of monographs. New York: Academic press; 1978. p. 325-57.
78. Hofmann K. Imidazole and it's derivatives. Chemistry of Heterocyclic compounds. New York: Interscience Publishers; 1953. p. 247-324.
79. Tsukamoto G, Yoshino K, Kohno T, Ohtaka H, Kagaya H, Ito K. Synthesis and antiinflammatory activity of some 2-(substituted-pyridinyl)benzimidazoles. J Med Chem. 1980 Jul;23(7):734-8.
80. Ito K, Kagaya H, Satoh I, Tsukamoto G, Nose T. The studies of the mechanism of antiinflammatory action of 2-(5- ethylpyridin-2-yl)benzimidazole (KB-1043). Arzneimittelforschung. 1982;32(2):117-22.
81. Ito K, Kagaya H, Fukuda T, Yoshino K, Nose T. Pharmacological studies of a new nonsteroidal antiinflammatory drug: 2- (5-ethylpyridin-2-yl)benzimidazole (KB-1043).Arzneimittelforschung. 1982;32(1):49-55.
82. Gilman SC, Carlson RP, Chang J, Lewis AJ. The antiinflammatory activity of the immunomodulator Wy-18,251 (3-(p- chlorophenyl)thiazolo[3,2-a]benzimidazole-2-acetic acid). Agents Actions. 1985;17(1):53-9.
83. Gilman SC, Carlson RP, Lewis AJ. Immunomodulatory activity of Wy-18,251 (3-(pchlorophenyl).Immunopharmacol.1985;7(1):79-98.
84. Lazer ES, Matteo MR, Possanza GJ. Benzimidazole derivatives with atypical antiinflammatory activity. J Med Chem. 1987;30(4):726-9.
85. Taniguchi K, Shigenaga S, Ogahara T, Fujitsu T, Matsuo M. Synthesis and antiinflammatory and analgesic properties of 2-amino-1H- benzimidazole and 1,2- dihydro-2-iminocycloheptimidazole derivatives. Chem Pharm Bull (Tokyo). 1993;41(2):301-9.
86. Boido A, Vazzana I, Sparatore F, Cenicola ML, Donnoli D, Marmo E. Preparation and pharmacological activity of some 1-lupinylbenzimidazoles and 1-lupinylbenzotriazoles. Farmaco. 1991 Jun;46(6):775-88.
87. Da Settimo F, Primofiore G, Da Settimo A, La Motta C, Taliani S, Simorini F, et al. [1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors. J Med Chem. 2001;44(25):4359-69.
88. Vogal AI. A Textbook of Practical Organic Chemistry. 3rd ed. London: ELBS & Longman Ltd; 1975. p. 225-36.
89. Copeland RA, Day AR. The preparation and reactions of 2-Benzimidazole carboxylic acid and 2-Benzimidazoleacetic acid. Journal of American Chemical Society. 1943;65:1072-5.
90. Rastogi R, Sharma S, Iyer RN. Synthesis of benzimidazole-2-carboxamides as potential anti-histaminic agents. Indian Journal of Chemistry. 1979;18B(464-467).
91. Phillips MA. Preparation of benzimidazoles. Journal of Chemical Society. 1928:174-5.
92. Organization for Economic Co-operation and Development. Guidance Document on Acute Oral Toxicity Testing. Paris Environment Directorate, OECD; 2001.
93. Winter CA, Risley EA, Nuss WG. Carrageenin-induced edema in hind paw of the rats as an assay for anti-inflammatory drugs.Proceedings of the Society for Experimental Biology and Medicine. 1962;111:544-7.
94. Hubert JJ, Bohider NR, Peace KE. Regression analysis. In: Peace KE, editor. Biopharmaceutical Statistics for Drug Development. Basel & New York: Marcel Dekker; 1992. p. 1-20.
95. Lagorce JF, Fatimi J, Lakhdar M, Chabernaud ML, Buxeraud J, Raby C. Synthesis and inhibitory effects of 2-pyridyl-2-thiobenzoxazole and 2-pyridyl-2-thiobenzimidazole derivatives on arachidonic acid metabolism. Arzneimittelforschung. 1995 Nov;45(11):1207-10.
96. Vane JR. Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nature: New biology. 1971 Jun 23;231(25):232-5.
97. Vane JR, Botting RM. The mechanism of action of aspirin. Thrombosis research. 2003 Jun 15;110(5-6):255-8.
98. Vane JR, Botting RM. Anti-inflammatory drugs and their mechanism of action. Inflamm Res. 1998 Oct;47 Suppl 2:S78-87.
99. Vane JR, Bakhle YS, Botting RM. Cyclooxygenases 1 and 2. Annual review of pharmacology and toxicology. 1998;38:97-120.
100. Claria J, Romano M. Pharmacological intervention of cyclooxygenase-2 and 5- lipoxygenase pathways. Impact on inflammation and cancer. Current pharmaceutical design. 2005;11(26):3431-47.
101. Julemont F, Dogne JM, Pirotte B, de Leval X. Recent development in the field of dual COX / 5-LOX inhibitors. Mini reviews in medicinal chemistry. 2004 Aug;4(6):633-8.
102. Vane J, Botting R. Inflammation and the mechanism of action of anti-inflammatory drugs. Faseb J. 1987 Aug;1(2):89-96.
103. Eleni P, Dimitra HL. Review in quantitative structure activity relationships on lipoxygenase inhibitors. Mini reviews in medicinal chemistry. 2003 Aug;3(5):487.
104. Ruwart MJ, Nezamis JE, Rush BD, Lancaster C, Davis JP, Nichols NM, et al. Timoprazole is a unique cytoprotective agent in the rat. Digestion. 1984;30.
105. Musser JH, Kubrak DM, Chang J, DiZio SM, Hite M, Hand JM, et al. Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters. Med Chem. 1987 Feb;30(2):400
106. Skelly MM, Hawkey CJ. COX-LOX inhibition: current evidence for an emerging new therapy. International journal of clinical practice. 2003 May;57(4):301-4.
107. Rainsford KD. The ever-emerging anti-inflammatories. Have there been any real advances? Journal of physiology, Paris. 2001 Jan-Dec;95(1-6):11-9.
108. Rainsford KD. Mechanisms of gastrointestinal damage by NSAIDS. Agents and actions. 1993;44:59-64.
109. Crowther AF, Curd FHS, Davey DG, Stacey CJ. Synthetic antimalerials Part XXXIX: 5(or 6)-Chloro-2-hydroxymethyl benzimidazole. Journal of Chemical Society. 1949;49:1260-71.
110. Chatterjee B. CCCC.-Attempts to find new antimalerials. Part IV. Beta- Benzimidazolylethylamine and beta-5(or 6)-Ethoxybenzimidazolylethylamine. Journal of Chemical Society. 1929:2965-668.
111. James AT, Turner EE. Structure and antimelerial activity. Part IV. Benzimidazoles and mercaptodihydroglyoxalines. Journal of Chemical Society. 1950:1515-9.
112. Alp, M., Goker, H., Brun, R., Y?ld?z, S. (2009). Synthesis and anti-parasitic and anti-fungal evaluation of 20- arylsubsti-tuted-1H, 10H-[2, 50] bisbenzimidazolyl-5-carboxamidines.Eur.J.Med.Chem. 44:2002–2008. DOI PMid:19010569
113. Ansari, K.F., Lal, C (2009). Synthesis, physicochemical properties and anti-microbial activity of some new benzi-midazole derivatives. Eur. J. Med. Chem. 44: 4028–4033. DOI PMid:19482384.
114. Budow, S., Kozlowska, M., Gorska, A., Kazimierczuk, Z., Eickmeier, H., Colla, P.L.,Gosselin, G., Seela, F. (2009). Substituted benzimidazoles: anti-viral activity and synthe-sis of nucleosides. ARKIVOC iii: 225- 250.
115. Camacho J., Barazarte A., Gamboa N., Rodrigues J., Rojas R., Vaisberg A., Gilman R., Charris J. (2011). Synthesis and biological evaluation of benzimidazole-5-Carbohydrazide derivatives as anti-malarial, cytotoxic and anti-tubercular agents. Bioorg. & Med. Chem.19: 2023–2029. DOI
116. Cong, C.,Wang, H., Huc, C., Liu, C., Ma, S., Li, X.,Cao, J., Ma, S. (2011). Synthesis and anti-bacterial activity of novel 400-O-benzimidazolyl clarithromycin Derivatives. Eur. J. Med. Chem. 46:3105-3111. DOI PMid:21524827
117. Cvetkovic, S.O.P.K.D.D. (2011). Lipophilicity and anti-fungal activity of some 2-substituted benzimidazole derivatives. Chem. Ind. & Chem. Eng. Quart. 17 (1):9-15. DOI
118. Dandia, A., Singh, R., Merienne, C., Morgant, G., Loupy, A. (2006). Efficient microwave Enhanced regioselective synthesis of a series of benzimidazolyl/triazolyl spiro [indole-thiazolidinones] as potent anti-fungal agents and crystal structure of spiro[3H-indole-3, 20- thiazolidine]-30(1, 2,4-triazol-3-yl)- 2,40(1H)-dione. Bioorg. & Med. Chem. 14: 2409–2417. DOI
119. Elnima, E.I., Zubair, M., Badar, A.A. (1981). Anti-bacterial and antifungal activities of benzimidazole and benzox-azole derivatives. Antimicrob. Agents Chemother. 19(1):29-32. PMid:7247359 PMCid:181352.
120. Fang, B., Zhou, C.H., Rao, X.C. (2010). Synthesis and biological activities of novel amine-derived bis-azoles as potential anti-bacterial and anti-fungal agents. Eur. J. Med. Chem. 45: 4388-4398. DOI PMid:20598399.
121. Gomez H.T., Nunez E.H., Rivera I.L., Alvarez J.G., Rivera R.C., Puc R.M., Ramos A.R., Gutierrez, M.D.R., Bacab, M.J.C. Vazquez, G.N. (2008). Design, synthesis and in vitro anti-protozoal activity of benzimidazole- pentamidine hybrids. Bioorg. & Med. Chem. Lett. 18: 3147–3151. DOI Grocer, H., Kus, C., Boykin, D.W., Yildiz, S., Altanlar, N. (2002). Synthesis and Anti-fungal Properties of Some Benzimidazole Derivatives. Bioorg. Med. Chem.10:2589–2596. PMid:12057648.
122. Grocer, H., Kus, C., Boykin, D.W., Yildiz, S., Altanlar, N. (2002). Synthesis and Anti-fungal Properties of Some Benzimidazole Derivatives. Bioorg. Med. Chem.10:2589–2596. PMid:12057648 Gupta, H.C., Jaiswal, V. (2010). Synthesis and Anti-viral Activity of Some New benzimidazoles. J. Ind. Council Chem. 27(2):159-162.
123. Haugwitz, R.D. (1982). Anti-parasitic agents Synthesis and anti-helmintic activities of novel 2-substituted isothiocya-natobenzoxazoles and benzimidazole. J. Med. Chem. 25: 969-974. DOI PMid:7120286.
124. Kazimierczuk, Z., Upcroft, J.A., Upcroft, P., Gorska, A., Starosciak, B., Laudy, A. (2002). Synthesis and antiproto-zoal activity of some 2-(trifluoromethyl)-1H-benzimidazole bioisosteres. Acta.Biochim.Pol. 49: 185–195. PMid:12136939 Kilcigil, G.A., Altanlar. (2006). Synthesis and anti-fungal properties of some benzimidazole derivatives. Turk J. Chem. 30:223-228.
125. Kumar, B.V.S., Vaidya, S.D., Kumar, R.V., Bhirud, S.B., Mane, R.B. (2006). Synthesis and anti-bacterial activity of some novel 2-(6-fluorochroman-2-yl)-1-alkyl/acyl/aroyl-1H-benzimidazoles. Eur. J. Med. Chem. 41:599–604. DOI PMid:16527375.
126. Kumar, R.V., Vaidya, S.D., Kumar, B.V.S., Bhise, U.N., Bhirud, S.B., Mashelkar, U.C. (2008). Synthesis, anti- bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H- benzimidazoles and N-substituted,2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1Hbenzimidazoles. Eur. J. Med. Chem. 43:986-995. DOI PMid:17825955 Liu, S., Nelson, A.C., Xiao, L., Lu, L., Seth, P.P., Davis, D.R., Hagedorn, C.H. (2011). Measuring antiviral activity of benzimidazole molecules that alter IRES RNA structure with an infectious hepatitis C virus chimer expressing Renilla luciferase. Anti-viral Res. 89:54–63. DOI PMC-id:3018537.
127. Olmo, E.D., Barboza, B., Chiaradia, L.D., Moreno, A., Lerida, J.C., Pacanowska, D.G., Victoria, M., Perez, J.L.L., Giménez, A., Benito, A., Martinez, A.R., Perez, L.M.R.A., Feliciano, A.S. (2011). Anti-malarial activity of imidazo [2, 1- a] isoindol-5-olderivatives and related compounds. Eur. J. Med. Chem. 46:5379- 5386. DOI PMid:21940072 Patil, A., Ganguly, S., Surana, S. (2008). A systemic review of benzimidazole derivatives as an antiulcer agent. Rasayan Journal of Chemistry, 1(3): 447-460.
127. Ryckebusch A., Fontaine M.A.D., Mouray E., Grellier P., Sergheraerta C., Melnyk P. (2005). Synthesis and anti-malarial evaluation of new N1-(7-chloro-4-quinolyl)-1, 4-bis (3-aminopropyl)-piperazine derivatives. Bioorg. & Med. Chem. Lett.15: 297–302. DOI
128. Sharma, S., Gangal, S., Rauf, A. (2009). Convenient one-pot synthesis of novel 2-substituted benzimidazoles, tetrahy-drobenzimidazoles and imidazoles



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