151091-52-0Relevant articles and documents
Structure-activity relationships within a series of analogues of the histamine H1-antagonist terfenadine
Zhang,Ter Laak,Timmerman
, p. 165 - 173 (2007/10/02)
A number of terfenadine derivatives including terfenadine enantiomers were synthesized and tested for histamine H1-receptor affinity. No significant differences in H1 activity were found between terfenadine enantiomers. Qualitative structure-activity relationship studies identified the α,α-diphenyl-4-piperidinomethanol moiety as the pharmacophore for the H1 activity of this group of compounds. The major role of the phenylbutanol moiety in terfenadine seems to be preventing the compound from crossing the blood-brain barrier.