You are herePHARMACOLOGICAL ACTIVITIES OF BENZIMIDAZOLE- A REVIEW
PHARMACOLOGICAL ACTIVITIES OF BENZIMIDAZOLE- A REVIEW
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 .
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.
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.
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.
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  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. A series of benzamides has been synthesized with N – acridin -9-yl substituent.
Some compounds possessing dihydrochlorides have also been reported possessing antioxidant activity, these salts also possess mild platelet and erythrocyte antiaggregant activity. In another approach it was found out that using trimethyl group with benzimidazole also adds antioxidative property by 5-lipoxygenase inhibitory action.
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.
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
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