Rational design of a pirinixic acid derivative that acts as subtype-selective PPARγ modulator
Peroxisome proliferator-activated receptor γ (PPARγ) is involved in glucose and lipid homeostasis. PPARγ agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARγ modulators (SPPARγMs) was developed, which are believed to show less side effects than full PPARγ agonists. We have previously shown that α-substitution of pirinixic acid, a moderate agonist of PPARα and PPARγ, leads to low micromolar active balanced dual agonists of PPARα and PPARγ. Herein we present modifications of pirinixic acid leading to subtype-selective PPARγ agonists and furthermore the development of a selective PPARγ modulator guided by molecular docking studies.
Antiinflammatory activity of isomeric phenylnaphthaleneacetic acids
The isomeric phenylnaphthaleneacetic acids were prepared and tested for antiinflammatory activity by the anti-UV-erythema method. High potency was exhibited by 4- and 5-phenyl-1 naphthaleneacetic acid and 5- and 6-phenyl-2-naphthaleneacetic acid. The results are discussed in terms of a hypothetical receptor site.
Kaltenbronn
p. 596 - 598
(2007/10/13)
4- and 5-Aryl-l-naphthaleneacetic acids as antiinflammatory agents.
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Kaltenbronn
p. 490 - 493
(2007/10/13)
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