Synthesis of 5-Amido-1H-imidazopyridine Derivatives and Their AngiotensinⅡ Receptor Antagonistic Activities

Abstract

Abstract: AngiotensinⅡ(AⅡ) receptor antagonists are clinically useful for the management of cardiovascular disease. Based on the analysis of the quantitative structure-activity relationships of forty-two new compounds reported in literatures as AⅡ receptor antagonists, a series of novel 5-amido-1H-imidazopyridine derivatives were designed and synthesized by application of the methods of computer aided drug design and principles of bioisosterism and hybridization. All of them were first reported and their structures were confirmed by IR, ¹H NMR and MS spectra. The results of preliminary pharmacological tests in vitro show that some target compounds have certain antagonistic activity of AⅡ receptor. Moreover, the analysis of SAR suggests that N-phenylpyrrole-2-tetrazole can be used as a substitution for future designing of novel AⅡreceptor antagonists.

Key words: 5-Amido-1H-imidazopyridine derivatives, Synthesis, AⅡreceptor antagonistic activity, Antihypertensive, Heart failure

CLC Number:

O626

TrendMD:

XU Jin-Yi, HUA Wei-Yi, WU Xiao-Ming, WANG Qiu-Juan, HU Song. Synthesis of 5-Amido-1H-imidazopyridine Derivatives and Their AngiotensinⅡ Receptor Antagonistic Activities[J]. Chem. J. Chinese Universities, 2005, 26(6): 1067.

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Synthesis of 5-Amido-1H-imidazopyridine Derivatives and Their AngiotensinⅡ Receptor Antagonistic Activities

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