Bioorganic & Medicinal Chemistry Letters 29 (2019) 631–637 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR a,1 a a a a a Wonken Choung , Hui Jin Jung , Deokmo Yang , Eun Hye Nam , Hyukjoon Choi , Bo Ram Lee , a a a a b b Min Park , Su Min Jang , Jae Soo Lim , Woo Sik Kim , Kyung-Hee Kim , Jungwook Chin , b b b b a Kyungjin Jung , Geumwoo Lee , Eunmi Hong , Tae-ho Jang , Jayhyuk Myung , a, ,1 Seong Heon Kim Research Center, Boryung Pharmaceuticals Co. Ltd., Republic of Korea New Drug Development Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Republic of Korea ARTICLE INFO ABSTRACT Keywords: The new class of PPARgamma non-TZD agonist originally derived from the backbone of anti-hypertensive Drug discovery Fimasartan, BR101549, was identified as a potential lead for anti-diabetic drug development. The X-ray crys- Antidiabetics tallography of BR101549 with PPARgamma ligand binding domain (LBD) revealed unique binding character- PPARgamma agonist istics versus traditional TZD full
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Feb 15, 2019
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