European Journal of Medicinal Chemistry

GABA uptake inhibitors. Syntheses and structure—activity studies on GABA analogues containing diarylbutenyl and diarylmethoxyalkyl N-substituents

E Falch, P Korgsgaard-Larsen

文献索引：Falch; Krogsgaard-Larsen European Journal of Medicinal Chemistry, 1991 , vol. 26, # 1 p. 69 - 77

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被引用次数: 25

摘要

Abstract A number of analogues of GABA or β-alanine containing 4, 4-diphenyl-3-butenyl (DPB), benzhydryl ethyl ether (BEE), or benzhydryl propyl ether N-substituents have been synthesized and tested as inhibitors of synaptosomal GABA uptake. Whereas the N-DPB and N-BEE analogues of GABA are markedly less potent than GABA itself as inhibitors of GABA uptake, N-methylation of these analogues resulted in increased potency and ...