Studies on Cerebral Protective Agents. VIII. Synthesis of 2-Aminothiazoles and 2-Thiazolecarboxamides with Anti-anoxic Activity
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概要
- 論文の詳細を見る
Various 2-aminothiazoles (2a-s and 3a-g) and 2-thiazolecarboxamides (4a-h), possessing a nitrogenous basic moiety at the C-2 position of the thiazole ring, were prepared and tested for anti-anoxic (AA) activity in mice. Among them, N-[2-(4-morpholinyl)ethyl]-4-(3-trifluoromethylphenyl)-2-thiazolecarboxamide hydrochloride (4e, FR108143) (minimum effectvie doses of 3.2 mg/kg i.p. and 10 mg/kg p.o., respectively) exhibited more potent AA activity than either FK360 or compound 1,each of which has a nitrogenous basic moiety at the C-5 position. The structure-activity relationships with regard to AA activity of this series of compounds are discussed, and the three-dimensional electrostatic potentials (3D-MEP) around the basic nitrogen atom of FK360 and the thiazole derivative (4e) are compared.
- 社団法人日本薬学会の論文
- 1995-09-15
著者
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大久保 充
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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仲西 功
Molecular Design Group Fujisawa Pharmaceutical Co., Ltd.,
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久野 敦司
New Drug Research Laboratories Fujisawa Pharmaceutical Co., Ltd.,
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仲西 功
R & D Information, Fujisawa Pharmaceutical Co., Ltd.,
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co., Ltd.,
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高杉 寿
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd
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Takasugi H
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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仲西 功
Molecular Design Group Fujisawa Pharmaceutical Co. Ltd.
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久野 敦司
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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Nakanishi Isao
New Drug Research Laboratories R & D Information Fujisawa Pharmaceutical Co. Ltd.
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