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

Mukesh C. Sharma, D. Kohli, Smita Sharma
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引用次数: 13

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 ZnCl2 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 1H NMR, 13C 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. Keywords: Benzimidazoles; Biphenyl Carboxylic acid; Angiotension-II.
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新型苯并咪唑衍生物4'-{5-氨基-2-[2-取代苯基氨基)-苯基甲基]-苯并咪唑-1基甲基}-联苯-2-羧酸的合成及生物学评价:非肽血管紧张素II受体拮抗剂
制备了一系列新的血管紧张素(A- ii)受体拮抗剂。以2-(α-羟基苯基)苯并咪唑为原料,与HBr反应生成2-(α-溴基)苯并咪唑,无水ZnCl2席夫碱与具有不同取代基氨基的联苯羧酸进行环缩合反应,合成了一些新的4'-{5-氨基-2-[2-取代苯基氨基]-苯基甲基]-苯并咪唑-1-基甲基}-联苯-2-羧酸衍生物。不同于先前报道的相关化合物,它们具有有效的降压作用。合成的化合物经1H NMR、13C NMR、FAB质谱和FT-IR光谱鉴定。采用尾袖法和直接测血压法对所研究化合物的降压活性进行了筛选。关键词:苯并咪唑;联苯羧酸;Angiotension-II。
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