Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.

@article{An2020DiscoveryAS,
  title={Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPAR$\gamma$/$\delta$ Modulators.},
  author={Seungchan An and Gyudong Kim and Hyun Jin Kim and Sungjin Ahn and Hyun Young Kim and Hyejin Ko and Young Eum Hyun and Mai-Thao Nguyen and Juri Jeong and Zijing Liu and Jinhe Han and Hongseok Choi and Jinha Yu and Ji Won Kim and Hyuk Woo Lee and Kenneth A. Jacobson and Won Jea Cho and yOUNG-MI Kim and Keon Wook Kang and Minsoo Noh and Lak Shin Jeong},
  journal={Journal of medicinal chemistry},
  year={2020}
}
Following our report that A3 adenosine receptor (AR) antagonist 1 exhibited a polypharmacological profile as a dual modulator of peroxisome proliferator-activated receptor (PPAR)γ/δ, we discovered a new template, 1'-homologated adenosine analogues 4a-4t, as dual PPARγ/δ modulators without AR binding. Removal of binding affinity to A3AR was achieved by 1'-homologation, and PPARγ/δ dual modulation was derived from the structural similarity between the target nucleosides and PPAR modulator drug… 
4 Citations
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