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源自血管紧张素II 1型受体（AT1R）拮抗剂菲马沙坦的AT1R和PPARγ双功能调节剂的发现。

Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.

作者信息

Choung Wonken, Jung Hui Jin, Nam Eun Hye, Yang Deokmo, Yoo Byoungwook, Choi Hyukjoon, Lee Bo Ram, Park Min, Jang Su Min, Lim Jae Soo, Kim Kyung-Hee, Chin Jungwook, Jung Kyungjin, Lee Geumwoo, Kim Seong Heon

机构信息

Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea.

New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2018 Oct 15;28(19):3155-3160. doi: 10.1016/j.bmcl.2018.08.036. Epub 2018 Aug 28.

DOI:10.1016/j.bmcl.2018.08.036
PMID:30177375
Abstract

Inspired by the well-known PPARγ partial agonism of angiotensin II type 1 receptor (AT1R) antagonists exemplified by an antihypertensive drug, Telmisartan, efforts to identify compounds with the dual activities have been pursued in order to control the two major metabolic disorders, hypertension and hyperglycemia simultaneously. Lead compound 18 derived from the AT1R antagonist, Fimasartan, has successfully presented the possibility to control the medical conditions by a single molecule.

摘要

受以抗高血压药物替米沙坦为代表的血管紧张素II 1型受体（AT1R）拮抗剂的著名PPARγ部分激动作用的启发，人们一直在努力寻找具有双重活性的化合物，以便同时控制高血压和高血糖这两种主要的代谢紊乱。源自AT1R拮抗剂菲马沙坦的先导化合物18已成功展现了通过单一分子控制病情的可能性。

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Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.源自血管紧张素II 1型受体（AT1R）拮抗剂菲马沙坦的AT1R和PPARγ双功能调节剂的发现。
Bioorg Med Chem Lett. 2018 Oct 15;28(19):3155-3160. doi: 10.1016/j.bmcl.2018.08.036. Epub 2018 Aug 28.
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