De Sign and Synthesis of 1, 2, 4??Oxadiazole Derivatives as Non??Steroidal 5α??Reductase Inhibitors

…, CL Chen, KC Wang, JW Chern

Index: Chang, Chih-Shiang; Kan, Wai Ming; Chen, Chiu-Liang; Wang; Chern, Ji-Wang Journal of the Chinese Chemical Society, 2002 , vol. 49, # 1 p. 83 - 89

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Abstract

Abstract The purpose of this study was to synthesize compounds in which the 1, 2, 4- oxadiazole moiety replaced the amide bond of ONO3805 and to evaluate its 5α-reductase inhibitory activity as a potential benign prostatic hyperplasia therapeutic target. Four 1, 2, 4- oxadiazole derivatives, 1, 2, 8, and 20, were evaluated in vitro against 5α-reductase of rat liver microsome. The prepared 1 and 2 possessed similar binding affinity (Ki) to that of ...