Design and Synthesis of 3, 5??Disubstituted??1, 2, 4??Oxadiazoles as Potent Inhibitors of Phosphodiesterase4B2

…, G Patel, L Vijayakrishnan, SG Dastidar…

Index: Kumar, Dalip; Patel, Gautam; Vijayakrishnan, Lalitha; Dastidar, Sunanda G.; Ray, Abhijit Chemical Biology and Drug Design, 2012 , vol. 79, # 5 p. 810 - 818

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Citation Number: 5

Abstract

A series of 3, 5-disubstituted-1, 2, 4-oxadiazoles has been prepared and evaluated for phosphodiesterase inhibition (PDE4B2). Among the prepared 3, 5-disubstituted-1, 2, 4- oxadiazoles, compound 9a is the most potent inhibitor (PDE4B2 IC50= 5.28 lM). Structure– activity relationship studies of 3, 5-disubstituted-1, 2, 4-oxadiazoles revealed that substituents 3-cyclopentyloxy-4-methoxyphenyl group at 3-position and cyclic ring bearing ...