Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
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.
['Choung|Wonken|W|', 'Jung|Hui Jin|HJ|', 'Nam|Eun Hye|EH|', 'Yang|Deokmo|D|', 'Yoo|Byoungwook|B|', 'Choi|Hyukjoon|H|', 'Lee|Bo Ram|BR|', 'Park|Min|M|', 'Jang|Su Min|SM|', 'Lim|Jae Soo|JS|', 'Kim|Kyung-Hee|KH|', 'Chin|Jungwook|J|', 'Jung|Kyungjin|K|', 'Lee|Geumwoo|G|', 'Kim|Seong Heon|SH|']
D047228:Angiotensin II Type 1 Receptor Blockers D000818:Animals D000959:Antihypertensive Agents D019540:Area Under Curve D001713:Biphenyl Compounds D004195:Disease Models, Animal D055808:Drug Discovery D054333:Drug Partial Agonism D006207:Half-Life D007004:Hypoglycemic Agents D047495:PPAR gamma D000075082:Proof of Concept Study D011743:Pyrimidines D013329:Structure-Activity Relationship D013777:Tetrazoles
PPARγ Fimasartan Antihypertensives Angiotensin II type 1 receptor antagonist Antidiabetics Drug discovery Dual modulator