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Modulation of PPAR subtype selectivity. Part 2: Transforming PPARα/γ dual agonist into α selective PPAR agonist through bioisosteric modification

✍ Scribed by Pandurang Zaware; Shailesh R. Shah; Harikishore Pingali; Pankaj Makadia; Baban Thube; Suresh Pola; Darshit Patel; Priyanka Priyadarshini; Dinesh Suthar; Maanan Shah; Jeevankumar Jamili; Kalapatapu V.V.M. Sairam; Suresh Giri; Lala Patel; Harilal Patel; Hareshkumar Sudani; Hiren Patel; Mukul Jain; Pankaj Patel; Rajesh Bahekar

Book ID: 104005216
Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 923 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.12.032

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ChemInform Abstract: Modulation of PPAR

ChemInform Abstract: Modulation of PPAR Subtype Selectivity. Part 2. Transforming PPARα/γ Dual Agonist into α Selective PPAR Agonist Through Bioisosteric Modification.

✍ Rajesh Bahekar; et al. et al. 📂 Article 📅 2011 🏛 John Wiley and Sons ⚖ 25 KB 👁 1 views

Bioisosteric replacement of the rigid oxazole ring of a previously reported PPARα/γ dual agonist with a flexible lipophilic tail leads to a series of oxime containing benzyl dioxanecarboxylic acid derivatives. Compounds (I) show high selectivity towards PPARα over PPARγ in vitro. Furthermore, the hi