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 |
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Authors: | Ohmori Yutaka Yamashita Akitake Tsujita Ryuichi Yamamoto Tamotsu Taniuchi Kaku Matsuda Akira Shuto Satoshi |
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Affiliation: | Institute for Life Science Research, Asahi Kasei Co, Ltd, Ohito-cho, Shizuoka 410-2321, Japan. |
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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. |
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