A Novel Class of Inhibitors for Human Steroid 5α-Reductase : Phenoxybenzoic Acid Derivatives. I

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概要

• 論文の詳細を見る

• In a search for novel nonsteroidal inhibitors of human prostatic 5α-reductase, we found a new series of phenoxybenzoic acid derivatives to be potent human prostatic 5α-reductase inhibitors. Among them, 4-(biphenyl-4-yloxy)benzoic acid derivatives (2n, YM-31758), 2o and 2s showed more potent inhibitory activities than finasteride with IC_<50> values of 0.87,0.67 and 0.56nM, respectively. The optimized structures for the phenoxybenzoic acid derivatives 2d-2i were calculated by molecular modeling analysis, and the favorable distance between the carbon of the carboxyl group and the centroid of the phenyl group (benzene ring C) was found to be in the 9-11Å range.

• 公益社団法人日本薬学会の論文
• 1999-08-15

著者

• Hara Hideaki

  Research And Development Center Santen Pharmaceutical Co. Ltd.

• Fujii M

  Samsung Yokohama Res. Inst. Co. Ltd. Yokohama‐shi Jpn

• Fujii M

  Tokyo University Of Science:(present Office)utsunomiya University

• Fujii M

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Fujii M

  Showa Univ. Tokyo Jpn

• IGARASHI Susumu

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• HARA Hiromu

  (Present Address)Secretariat Dept., Yamanouchi Pharmaceutical Co., Ltd.,

• FUJII Masahiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• KOUTOKU Hiroshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• ORITANI Hiroyuki

  (Present address)Institute for Drug Development Research, Yamanouchi Pharmaceutical Co., Ltd.,

• MASE Toshiyasu

  (Present address)Bulk Manufacturing & Technology Division, Yamanouchi Pharmaceutical Co., Ltd.,

• KIMURA Takenori

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• NAITO Ryo

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• Igarashi S

  Department Of Materials Science. Facnlty Of Engineering Ibaraki University

• Naito Ryo

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Hara H

  (present Address)corporate Planning Dept. Yamanouchi Pharmaceutical Co. Ltd.

• Mase T

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Koutoku Hiroshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Oritani Hiroyuki

  (present Address)institute For Drug Development Research Yamanouchi Pharmaceutical Co. Ltd.

• Kimura Takenori

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

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