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A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.

作者信息

Ohmori Yutaka, Yamashita Akitake, Tsujita Ryuichi, Yamamoto Tamotsu, Taniuchi Kaku, Matsuda Akira, Shuto Satoshi

机构信息

Institute for Life Science Research, Asahi Kasei Co, Ltd, Ohito-cho, Shizuoka 410-2321, Japan.

出版信息

J Med Chem. 2003 Dec 4;46(25):5326-33. doi: 10.1021/jm030226n.

DOI:10.1021/jm030226n
PMID:14640541
Abstract

A series of conformationally restricted analogues of milnacipran, a weak NMDA receptor antagonist, were designed by a method based on allylic strain. The conformational analysis study showed that the allylic-strain-based conformational restriction indeed occurred and that the affinity for the NMDA receptor was efficiently improved by the conformational restriction.

摘要

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