Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 24, Pages 10301-10310Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.10.040
Keywords
Benzimidazole derivatives bearing a heterocyclic ring; Nonpeptide angiotensin II receptor antagonists; Synthesis; Biological activity
Funding
- Chinese Academy of Sciences
- Diao Pharmaceutical Company
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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. (C) 2008 Elsevier Ltd. All rights reserved.
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