Novel highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulators with pharmacokinetic properties suitable for once-daily oral dosing

Autor:	Sunil Kumar Panigrahi, Effie Tozzo, Narasimha Rao Krishnamurthy, Taisuke Takahashi, Mahaboobi Jaleel, Nirbhay Kumar Tiwari, Bharat Lagu, Michael A. Patane, Ramesh S. Senaiar, Ross Fredenburg, Arthur F. Kluge
Rok vydání:	2017
Předmět:	0301 basic medicine Male Clinical Biochemistry Pharmaceutical Science Peroxisome proliferator-activated receptor Administration Oral Pharmacology Biochemistry 03 medical and health sciences chemistry.chemical_compound Mice Structure-Activity Relationship Pharmacokinetics Oral administration Drug Discovery Animals Humans Dosing Rats Wistar Benzamide Molecular Biology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Organic Chemistry Highly selective Multiple species Macaca fascicularis 030104 developmental biology chemistry Benzamides Injections Intravenous Molecular Medicine Once daily
Zdroj:	Bioorganicmedicinal chemistry letters. 27(23)
ISSN:	1464-3405
Popis:	Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral administration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f57037ac6e56607083a4697cf927ed4 https://pubmed.ncbi.nlm.nih.gov/29103972 Zobrazit plný text záznamu Full Text from ScienceDirect