Chemical and Pharmaceutical Bulletin p. 333 - 337 (1997)
Update date:2022-09-26
Topics:
Okada, Minoru
Yoden, Toru
Kawaminami, Eiji
Shimada, Yoshiaki
Kudoh, Masafumi
Isomura, Yasuo
1-N,N-Disubstituted amino-1H-1,2,4-triazole derivatives were prepared and evaluated for aromatase-inhibitory activity (in vitro) and for the inhibitory activity on pregnant mare serum gonadotropin (PMSG)-induced estrogen synthesis (in vivo). 1-N-para-Substituted benzylamino derivatives, having an electron-withdrawing group on the phenyl moiety, exhibited aromatase-inhibitory activity in vitro and in vivo. Among them, 1-[(4- nitrobenzyl)(4-nitrophenyl)amino]-1H-1,2,4-triazole (5b) was the most potent aromatase inhibitor. These 1-N-benzylamino derivatives also showed relatively strong inhibitory activity on aldosterone synthesis, indicating that the selectivity of these derivatives for aromatase inhibition was not sufficient in comparison with that of the 4-amino-4H-1,2,4-triazole derivatives.
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