Conformational Analysis of the NMDA Receptor Antagonist (1S,2R)-1-Phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide (PPDC) Designed by a Novel Conformational Restriction Method Based on the Structural Feature of Cyclopronane Ring
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概要
- 論文の詳細を見る
(1S,2R)-1-Phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide (2b, PPDC), a new class of potent N-methyl-D-aspartic acid (NMDA) receptor antagonist, was designed based on a new method for restricting the conformation of compounds having a cyclopropane ring. The three-dimensional structures of PPDC obtained by the three different methods of X-ray crystallographic analysis, usual MM2-calculations in vacuum, and MM2 calculations based on the nuclear Overhauser effect (NOE) data in D_2O are similar, which are in accord with that hypothesized. These results suggest that this conformational restriction method is particularly effective in designing novel biologically active molecules.
- 社団法人日本薬学会の論文
- 2002-07-01
著者
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小野 哲
富山化学工業株式会社綜合研究所
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Shuto S
Graduate School Of Pharmaceutical Sciences Hokkaido University
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Shuto Satoshi
Graduate School Of Pharmaceutical Sciences Hokkaido University
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OGAWA Kiyoshi
Institute of Plasma Physics,Nagoya University
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Matsuda A
Graduate School Of Pharmaceutical Sciences Hokkaido University
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Matsuda A
Faculty Of Pharmaceutical Sciences Hokkaido University
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Kazuta Yuji
Graduate School of Pharmaceutical Sciences, Hokkaido University
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Matsuda Akira
Graduate School of Pharmaceutical Sciences, Hokkaido University
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ONO Sizuka
Graduate School of Pharmaceutical Sciences, Hokkaido University
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YAMASHITA Kanako
Institute of Life Science Research, Asahi Chemical Co., Ltd.
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YAMAMOTO Tamotsu
Institute of Life Science Research, Asahi Chemical Co., Ltd.
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Ogawa K
Institute Of Life Science Research Asahi Chemical Co. Ltd.
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Matsuda Akira
Department Of Pharmaceutical Sciences Faculty Of Pharmaceutical Sciences
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Matsuda A
Hokkaido Univ. Sapporo
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Matsuda Akira
The Department Of Internal Medicine Kin-ikyo Chuo Hospital
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Ono S
Graduate School Of Pharmaceutical Sciences Hokkaido University
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Kazuta Yuji
Graduate School Of Pharmaceutical Sciences Hokkaido University
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Yamamoto T
Institute Of Life Science Research Asahi Chemical Co. Ltd.
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Yamashita K
Department Of Chemical Science And Technology Faculty Of Engineering The University Of Tokushima
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Matsuda Akira
Graduate School Of Pharmaceutical Sciences Hokkaido University
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Ogawa Kiyoshi
Institute For Life Science Research Asahi Chemical Industry Co. Ltd.
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Yamashita Kanako
Institute For Life Science Research Asahi Chemical Industry Co. Ltd.
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