Synthesis and biological evaluation of some new benzimidazoles derivatives 4'-{5-amino-2-[2-substituted-phenylamino)-phenyl-methyl]-benzimidazol-1 ylmethyl}-biphenyl-2-carboxylic acid: Nonpeptide angiotensin II receptor antagonists.

Abstract

A new series of non peptide angiotensin (A-II) receptor antagonist has been prepared. This N-(biphenyl methyl) imidazoles e.g. Some new 4'-{5-amino-2-[2-substituted-phenylamino)-phenyl-methyl]-benzimidazol-1-ylmethyl}-biphenyl-2-carboxylic acid derivatives were synthesized by 2-( α -hydroxy benzyl) benzimidazole was converted to 2-(α-bromo benzyl) benzimidazole by reacting with HBr and Anhydrous ZnCl 2 Schiff bases react with biphenyl carboxylic acid with different substituents amino group cyclocondensation with appropriate reagents. Differ from the previously reported and related compounds in that they produce a potent hypertensive effect. The compounds synthesized were identified by 1 H NMR, 13 C NMR, FAB Mass and FT-IR spectroscopic techniques. All compounds studied in this work were screened for their antihypertensive activity by tail cuff method and direct method measurement of blood pressure.

Comprehensive Review in Current Developments of Benzimidazole‐Based Medicinal Chemistry

“…Presence of amino group ( 224 ) has increased the activity substantially over the substituted one. The maximum activity has been observed with amino group .…”

“…Presence of amino group (224) has increased the activity substantially over the substituted one. The maximum activity has been observed with amino group (238,239). Compound (226) was as active as albendazole against T. spiralis.…”

Synthesis, Characterization, and Biological Evaluation of 2-(N-((2′-(2H-tetrazole-5-yl)-[1,1′-biphenyl]-4yl)-methyl)-pentanamido)-3-methyl Butanoic Acid Derivatives

“…The renin-angiotensin system plays a significant role in blood pressure control via the functions of angiotensin II which includes the release of nor-epinephrine, the secretion of aldosterone, the re-absorption of renal sodium, and vasoconstriction. Therefore, it can be considered a beneficial intervention in handling hypertension [ 4 ]. Among the hypertensive group of drugs, valsartan (2-(N-((2′-(2H-tetrazole-5-yl)-[1,1′-biphenyl]-4yl)-methyl)-pentanamido)-3-methyl butanoic acid) is one of the most commonly used drug moieties used in the treatment of hypertension [ 5 ].…”

Synthesis and characterization of novel mixed complexes derived from 2-aminomethylbenzimidazole and 2-(1H-Benzimidazol-2-yl) aniline and theoretical prediction of toxicity

“…In previous years, the research describing the importance of systems containing benzimidazole heterocyclic system was largely multiplied and covered vast bioactive activities including antimicrobial [1][2][3], antifungal 4, anti-inflammatory [5,6 ] antihelminthic [7], antitubercular 8,9, antithrombotic; antiplatelet and anticoagulant [10], antiulcer [11], antiprotozoal 12, antileishmanial 13, anti-inflammatory 14, antiviral 15 antimycobacterial 16, anti-HIV [17], antitumour [18]. Recently, benzimidazole target was reported as an anti-hypertensive agent [19,20], potent nonnucleoside reverse transcriptase inhibitors [21], inhibitors of the hepatitis C virus [22], anticonvulsant [23], ulcerogenic [24], nonpeptide angiotensin II receptor antagonists [25], potent activators of AMPactivated protein kinase [26] and antileukemic agents 27. R.V.…”