2. Academic Validation
  3. Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo

Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo

  • Eur J Med Chem. 2012 Jul:53:190-202. doi: 10.1016/j.ejmech.2012.03.055.
Jungyeob Ham 1,  Hoosang Hwang,  Euno Kim,  Jeong-Ah Kim,  Sung Jin Cho,  Jaeyoung Ko,  Woojin Lee,  Jaehwan Lee,  Harish Holla,  Joydeep Banerjee,  Seokho Kim,  Inho Yang,  Hyun Joo Lee,  Kyoungjin Shin,  Hyukjae Choi,  Sang-Jip Nam,  Jungae Tak,  Dongyup Hahn,  Taekyung Oh,  Dong Hwan Won,  Tae Gu Lee,  Jihye Choi,  Mi Sun Park,  Chaok Seok,  Jungwook Chin,  Heonjoong Kang
Affiliations

Affiliation

  • 1 Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul 151-747, Republic of Korea.
PMID: 22534184 DOI: 10.1016/j.ejmech.2012.03.055
Abstract

We have discovered and demonstrated the in vitro and in vivo PPARδ-selective activity of novel Y-shaped agonists. These compounds activated hPPARδ with EC(50) values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARδ agonists with 10(4)-fold selectivity over the Other two subtypes, namely, hPPARα and hPPARγ. The PPARδ ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.

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