Studies on Aromatase Inhibitors. II. Synthesis and Biological Evaluation of 1-Amino-1H-1,2,4-triazole Derivatives.

Authors:
  • TYToru Yoden
    Toru Yoden
  • EKEiji Kawaminami
    Eiji Kawaminami
  • MKMasafumi Kudoh
    Masafumi Kudoh
  • YIYasuo Isomura
    Yasuo Isomura
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Abstract
1-N,N-Disubstituted amino-1-H-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.