Studies on Topical Antiinflammatory Corticosteroids. I. Syntheses and Vasoconstrictive Activities of 11β, 17α, 21-Trihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione 17-Ester and 17,21-Diester Derivatives

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概要

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• Seven 17-ester and thirty-eight 17,21-diester compounds (3 and 4) of 11β, 17α, 21-trihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione (6α-methylprednisolone, 1) were synthesized and thirty-eight selected compounds were tested for vasoconstrictive activity in humans. Except for 4g_1 and 4g_2,they were more active than the mother compound (1). In particular, the activities of ten compounds (3b-g, 4b_<9,10>, 4c_<2,3>, and 4c_6) were equal to or greater than that of 9α-fluoro-11β, 21-dihydroxy-16β-methyl-17α-valeryloxy-1,4-pregnadiene-3,20-dione (betamethasone 17-valerate, BV). The activities of 21-methoxyacetate compounds (4b_9,4c_6 and 4d_5) were potent. The structure-activity relationship is discussed.

• 社団法人日本薬学会の論文
• 1985-05-25

著者

• 池上 四郎

  Faculty of Pharmaceutical Sciences, Teikyo University

• 内藤 泰男

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 梶原 良夫

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 吉田 誠一郎

  Research Laboratories, Ohta Pharmaceutical Co., Ltd.

• 菅井 三郎

  Research Laboratories, Ohta Pharmaceutical Co., Ltd.

• 神原 俊文

  Research Laboratories, Ohta Pharmaceutical Co., Ltd.

• 赤星 三彌

  Research Laboratories, Ohta Pharmaceutical Co., Ltd.,

• 釜野 徳明

  Cancer Research Institute, Arizona State University

• 岡崎 徳二

  Research Laboratories, Ohta Pharmaceutical Co., Ltd.,

• 釜野 徳明

  Cencer Reseach Institute And Department Of Chemistry Arizona State University

• 赤星 三彌

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 池上 四郎

  Faculty Of Pharmaceutical Sciences Teikyo University

• 吉田 誠一郎

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 菅井 三郎

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 神原 俊文

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

• 岡崎 徳二

  Research Laboratories Ohta Pharmaceutical Co. Ltd.

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