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2-Amino-6-chloro-4-(N-methylpiperazino) pyrimidines, Inhibitors of spiroperidol binding

C Gueremy, F Audiau, A Uzan, G Le Fur…

文献索引:Gueremy, Claude; Audiau, Francois; Uzan, Andre; Fur, Gerard Le; Leger, Jean-Michel; Carpy, Alain Journal of Medicinal Chemistry, 1982 , vol. 25, # 12 p. 1459 - 1465

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被引用次数: 11

摘要

A series of 30 6-chloro-2, 4-diaminopyrimidines was synthesized and tested in vitro as inhibitors of [3H] spiroperidol binding. The affinity for the dopamine receptor was shown to be related to the 6-chloro-4-(N-methylpiperazine) pyrimidine structure bearing a NH2 or NHRl group as a substituent in position 2, provided that R1 was not an a branched alkyl group. The nature of the substituent in position 5 is also of importance for the affinity; 2-( ...