Synthesis of Benzimidazole Derivatives: As Anti-hypertensive Agents

Abstract

A new series of non peptide angiotensin(A-II) receptor antagonist has been prepared. ThisN-(biphenyl methyl) imidazolese.g. 5-substituted (amino) -2- phenyl-1-(2ʼcarboxy biphenyl-4-yl) benzimidazoles differ from the previously reported and related compounds in that they produce a potent hypertensive effect upon oral administration. The earlier series were generally active only when administered intravenously. It has been found that 2’-position of biphenyl is essential. Only ortho substituted acid possess both high affinity for the AII receptor and oral anti-hypertensive potency.

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“…Several substituted and condensed benzimidazoles have been reported to exhibit an array of biological activities which include antimicrobial [1][2][3] , antiviral 4 , antiprotozoal 5 , anti-hypertensive 6 , antiallergic 7 , antioxidant, anti-allergic, analgesic, anti-inflammatory 8 activities and so on. Based upon the fact, the present investigation was planned substantial and interest has been shown in the synthesis and characterization of benzimidazole compounds in search of potential drugs.…”

Antibacterial Screening of New Synthesis Schiff Base having Benzimidazole Moiety

“…Benzimidazole is a versatile pharmacophore producing a different range of biological activities [2], including analgesic [3] and antiinflammatory [4][5][6]. Benzimidazole derivatives have found the application in different therapeutic areas including, antihypertensive [7], antiviral [8,9], antifungal [10][11][12], anticancer [13][14][15], antitubercular [16,17], antioxidant [18,19], antimicrobial [20][21][22][23], antibacterial [24][25][26]. Benzimidazole derivatives are highly active against several viruses such as HIV, herpes (HSV-1), RNA, influenza and human cytomegalovirus (HCMV) [27].…”

Synthesis, Characterization and Antibacterial Evaluation of some Novel Benzimidazole Derivatives Containing 1,3,4-Thiadiazole Moiety.

“…1,2 Benzimidazole ring count a significant heterocyclic pharmacophore in the drug discovery, these compounds which carrying diverse substituents in the structure of benzimidazole are associated with a wide range of biological activities including: antifungal, 3,4,5 anticancer, 6,7,8 antiinflammatory, 9,10 antioxidant, 11,12,13 anti-bacterial, 14,15,16,17 anti-viral, 18,19 anticoagulant, 20 and anti-hypertensive properties. 21 Despite of many attempts to develop and discover new structural type in the search for great and more effective antimicrobials, benzimidazoles still consider as one of the most versatile and significant type of compounds against microbes. 22,23 The benzimidazole containing compounds as a structural motif have been widely used in medicinal chemistry and drugs development.…”