301533-59-5Relevant articles and documents
Design, Synthesis, and Biological Evaluation of 6-Benzoxazole Benzimidazole Derivatives with Antihypertension Activities
Wu, Zhuo,Bao, Xiao-Lu,Zhu, Wei-Bo,Wang, Yan-Hui,Phuong Anh, Nguyen Thi,Wu, Xiao-Feng,Yan, Yi-Jia,Chen, Zhi-Long
, p. 40 - 43 (2019/01/14)
A series of new angiotensin II receptor 1 antagonists were prepared. They displayed nanomolar affinity to AT1 receptor and could decrease blood pressure efficiently in spontaneously hypertensive rats. Among them, compounds 1b and 2b could reduce the blood pressure with more or equal potency compared to Losartan. So, compounds 1b and 2b could be considered as potential antihypertension drug candidates.
Facile Synthesis of Novel Nonpeptide Angiotensin II Receptor Antagonists
Yang, Ling-Chun,Qi, Chuan-Min,Zhang, Guan-Xin,Zou, Nan-Zhi
, p. 1107 - 1112 (2007/10/03)
A series of Losartan analogues 1-12 with different functional groups were synthesized and characterized. In comparison with the previous reports, the synthetic procedures described in this paper have been optimized as follows below: 1) preparation of aromatic amine 15 and 18 through hydrogenation by employing Raney Ni and hydrazine as catalysts in place of palladium; 2) preparation of nitro-compound 17 by using pure fuming nitric acid at -20 - -15°C; 3) alkylation of 21 with 22 or 23 in the presence of sodium hydride in place of potassium tert-butylate; 4) preparation of carboxylic acid 4 by ester cleavage rather than hydrolysis of cyano group.