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 ...