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

[Display omitted] •A lead compound with dual activity for PPARγ and AT1R has been identified.•Extensive SAR on antihypertensive Fimasartan led to the lead, Compound 18.•Lead has proved its POC in animal models of type 2 diabetes and hypertension, respectively. Inspired by the well-known PPARγ partia...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-10, Vol.28 (19), p.3155-3160
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Angiotensin II type 1 receptor antagonist Angiotensin II Type 1 Receptor Blockers - chemistry Angiotensin II Type 1 Receptor Blockers - pharmacokinetics Angiotensin II Type 1 Receptor Blockers - pharmacology Animals Antidiabetics Antihypertensive Agents - chemistry Antihypertensive Agents - pharmacokinetics Antihypertensive Agents - pharmacology Antihypertensives Area Under Curve Biphenyl Compounds - chemistry Biphenyl Compounds - pharmacokinetics Biphenyl Compounds - pharmacology Disease Models, Animal Drug Discovery Drug Partial Agonism Dual modulator Fimasartan Half-Life Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacokinetics Hypoglycemic Agents - pharmacology PPAR gamma - agonists PPARγ Proof of Concept Study Pyrimidines - chemistry Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Structure-Activity Relationship Tetrazoles - chemistry Tetrazoles - pharmacokinetics Tetrazoles - pharmacology
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!