1239196-56-5Relevant articles and documents
Design, synthesis and biological evaluation of AT1 receptor blockers derived from 6-substituted aminocarbonyl benzimidazoles
Wu, Zhuo,Anh, Nguyen Thi Phuong,Yan, Yi-Jia,Xia, Ming-Bao,Wang, Yan-Hui,Qiu, Yan,Chen, Zhi-Long
, (2019)
A series of new 6-substituted aminocarbonyl benzimidazole derivatives with 1, 4-disubsituted or 1, 5-disubsituted indole moiety and benzoic acid moiety were designed, synthesized and pharmacologically evaluated. Most of the synthesized compounds could bind to the AT1 receptor and decrease blood pressure significantly. Notably, 2e and 1h could obviously decrease MBP in a dose dependent manner. The maximal response lowered 57.9 ± 2.3 mmHg (2e) and 57.6 ± 1.9 mmHg (1h) of MBP at 10 mg/kg after oral administration, and the antihypertensive effect lasted beyond 24 h, which performed better than Losartan (Fig. 1). These results indicate that 2e and 1h are effective and long-lasting anti-hypertension drug candidates and deserve further investigation for therapeutic application.
Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT1 receptor antagonists
Zhang, Jun,Wang, Jin-Liang,Zhou, Zhi-Ming,Li, Zhi-Huai,Xue, Wei-Zhe,Xu, Di,Hao, Li-Ping,Han, Xiao-Feng,Fei, Fan,Liu, Ting,Liang, Ai-Hua
, p. 4208 - 4216 (2012/08/28)
A series of 6-substituted carbamoyl benzimidazoles were designed and synthesised as new nonpeptidic angiotensin II AT1 receptor antagonists. The preliminary pharmacological evaluation revealed a nanomolar AT1 receptor binding affinity for all compounds in the series, and a potent antagonistic activity in an isolated rabbit aortic strip functional assay for compounds 6f, 6g, 6h and 6k was also demonstrated. Furthermore, evaluation in spontaneous hypertensive rats and a preliminary toxicity evaluation showed that compound 6g is an orally active AT1 receptor antagonist with low toxicity.
