A SHORT REVIEW ON POTENTIAL ACTIVITIES OF BENZIMIDAZOLE DERIVATIVES

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ABOUT AUTHOR:
Balram Soni*
Psychiatric Centre, S.M.S. Medical College,
Jaipur, Rajasthan, India
brpharma@rediffmail.com

ABSTRACT
Benzimidazole derivatives have shown hopeful activity in the treatment of several diseases, for this reason, the synthesis of novel benzimidazole remains a main focus for researchers. This review article summarizes the chemistry of different derivatives of benzimidazole along with their biological activities. The review article also covers the most active benzimidazole derivatives that have shown considerable pharmacological actions.

REFERENCE ID: PHARMATUTOR-ART-2227

PharmaTutor (ISSN: 2347 - 7881)

Volume 2, Issue 8

Received On: 04/06/2014; Accepted On: 17/06/2014; Published On: 01/08/2014

How to cite this article: B Soni; A Short Review on Potential Activities of Benzimidazole Derivatives; PharmaTutor; 2014; 2(8); 110-118

INTRODUCTION
Benzimidazoleis a heterocyclic aromatic organic compound. It is an important pharmacophore and a privileged structure in medicinal chemistry. Nowadays is a moiety of choice which possesses many pharmacological properties. The most prominent benzimidazole compound in nature is N-ribosyl-dimethylbenzimidazole, which serves as an axial ligand for cobalt in vitamin B12.[1]

The use of benzimidazole dates many years back for study of structural modifications and their pharmacological actions. Various benzimidazole derivatives were synthesized with the substitution of fluorine, propylene, tetrahydroquinoline which resulted in compounds with increased stability, bioavailability and significant biological activity.[2-3] In light of the affinity they display towards a variety of enzymes and protein receptors, medicinal chemists would certainly classify them as privileged ‘sub-structures’ for drug designing. The incorporation of the nucleus is an important synthetic strategy in studies of drug discovery. In the past few decades, benzimidazole and its derivatives have received much attention due to their chemotherapeutic values.[4]

Benzimidazole derivatives play very efficient role in the medical field with plenty of useful therapeutic activities like anti-inflammatory[5], antimicrobial[6], Diuretic[7], antiviral[8], anticancer[9], Antiprotozoal[10], Antiulcer[11], anti-oxidant[12], Anti-Asthmatic[13], Anti-Diabetic[14], Cysticidal[15], Analgesic[16], antihypertensive[17], anthelmintics[18], anti-HIV[19], anti-convulsant[20], and spasmolytic[21] activity. Benzimidazole and its derivatives have been showing hopeful activity in the treatment of several diseases, for these reasons, they achieved much attention as important pharmacophore and privileged structure in medicinal chemistry.

In order to obtain more effective chemotherapeutic agents, a variety of reports have been presented on the synthesis and biological evaluation of novel benzimidazole derivatives. The literature survey revealed the importance of the substitutions at 1, 2 and 5 positions of the benzimidazole ring for their pharmacological activities.

This review summarizes to know about the different derivatives of benzimidazole with their pharmacological activities. The synthesis of novel benzimidazole derivatives remains a main focus of medicinal research.

Compounds Having Benzimidazole Nucleus
* As Oral Anticoagulants

Dabigatran is an oral anticoagulant drug that acts as a direct thrombin (factor IIa) inhibitor. It can be used for the prevention of stroke in patients with atrial fibrillation. The drug was developed as an alternative to warfarin, since it does not require maintenance of international normalized ratio or monitoring by frequent blood tests, while offering similar efficacy in preventing ischemic events. Dabigatran can also be used to prevent the formation of blood clots in the veins (deep venous thrombosis) in adults who have had an operation to replace a hip or knee.[22]

Dabigatran

* As Oral Antidiabetic
Oral hypoglycemic drugs are used only in the treatment of type 2 diabetes which is a disorder involving resistance to secreted insulin. The oral antidiabetic containing benzimidazole includes Rivoglitazone.[23]

Rivoglitazone

* As Oral Antiviral
Antiviral drugs are a class of medication used specifically for treating viral infections such as influenza, herpes virus, viral hepatitis, human cytomegalovirus(HCMV) and human immunodeficiency virus (HIV) etc. The  oral antiviral drug containing benzimidazole includes Maribavir which isused for the prevention and treatment of human cytomegalovirus (HCMV) disease in hematopoietic stem cell/bone marrow transplant patients. The oral antiviralcontaining benzimidazole includes Maribavir.[24]

Maribavir

* Drugs in HSDD
HSDD (hypoactive sexual desire disorder) is the most commonly reported female sexual complaint and characterized by a decrease in sexual desire that causes marked personal distress and/or personal difficulties. The benzimidazole drug used in HSDD is Flibanserin which is a 5-HT1A receptor agonist and 5-HT2A receptor antagonist used as a non-hormonal treatment for pre-menopausal women with HSDD that had initially been investigated as an antidepressant. The drug containing benzimidazole used in HSDD includes Flibanserin.[25-26]

Flibanserin

* As Anti-hypertensive
Antihypertensive are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. The anti-hypertensive containing benzimidazole is Candesartan and Telmisartan.

Candesartan is an angiotensin-II receptor antagonist used mainly for the treatment of hypertension. Candesartan is also available in a combination formulation with a low dose thiazide diuretic, invariably hydrochlorothiazide, to achieve an additive antihypertensive effect. Candesartan/hydrochlorothiazide combination preparations are marketed under various trade names.[27]

Candesartan

Telmisartanis an angiotensin-II receptor antagonist used in the management of hypertension.

Telmisartan

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