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

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概要

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• 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, -[(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.

• 公益社団法人日本薬学会の論文
• 1997-02-15

著者

• Okada M

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• KUDOH Masafumi

  Metabolic Diseases Research, Pharmacology Laboratories, Institute for Drug Discovery Research, Yaman

• Isomura Y

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• OKADA Minoru

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• YODEN Toru

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• KAWAMINAMI Eiji

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• ISOMURA Yasuo

  Medical Chemistry Research II, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co.,

• SHIMADA Yoshiaki

  Medicinal Chemistry Research III, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical C

• SHIMADA Yasuo

  Mitsuboshi Pharmacutical Co.

• Yoden T

  Institute For Technology Development Yamanouchi Pharmaceutical Co. Ltd.

• Shimada Y

  Mitsuboshi Pharmaceutical Co

• Kudoh Masafumi

  Drug Discovery Research Astellas Pharma Inc.

• Kawaminami Eiji

  Medicinal Chemistry Research Ii Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co.

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