Structure-activity relationships within a series of analogues of the histamine H 1-antagonist terfenadine

MQ Zhang, AM Ter Laak, H Timmerman

文献索引：Zhang; Ter Laak; Timmerman European Journal of Medicinal Chemistry, 1993 , vol. 28, # 2 p. 165 - 173

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被引用次数: 29

摘要

Abstract A number of terfenadine derivatives including terfenadine enantiomers were synthesized and tested for histamine H 1-receptor affinity. No significant differences in H 1 activity were found between terfenadine enantiomers. Qualitative structure-activity relationship studies identified the α, α-diphenyl-4-piperidinomethanol moiety as the pharmacophore for the H 1 activity of this group of compounds. The major role of the ...