Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.

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Matthews JM, Chen X, Cryan E, Hlasta DJ, Rybczynski PJ, Strauss K, Tang Y, Xu JZ, Yang M, Zhou L, Demarest KT

Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6773-8. Epub 2007 Oct 17.

PubMed ID

18029176 [ View in PubMed

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Abstract

A series of aminoindane derivatives were synthesized and shown to be potent PPARalpha agonists. The compounds were obtained as racemates in 12 steps, and tested for PPARalpha activation and PPARalpha mediated induction of the HD gene. SAR was developed by variation to the core structure as shown within. Oral bioavailability was demonstrated in a Sprague-Dawley rat, while efficacy to reduce plasma triglycerides and plasma glucose was demonstrated in db/db mice.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	120	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	190	N/A	N/A	Details