Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring |
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Authors: | Guo Xing-Zhou Shi Lin Wang Rui Liu Xiao-Xiao Li Bo-Gang Lu Xiao-Xia |
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Affiliation: | Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, PR China. |
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Abstract: | A series of benzimidazole derivatives bearing a heterocyclic ring imidazole (1), 5-chloroimidazole (2), 1,2,4-triazol (3), and imidazoline (4) were synthesized and evaluated for angiotensin II antagonistic activities. The synthetic compounds 1-4 were biologically evaluated in vitro using an AT(1) receptor binding assay, where compounds 1 and 3 provided weak binding affinity, compound 2 showed moderate binding affinity, and compound 4 showed good binding affinity. Moreover, compound 4 was found to be almost equipotent with telmisartan in vivo biological evaluation study. |
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