Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H1-receptor agonists

S. Elz, K. Kramer, H.H. Pertz, M. Detert, A.M. ter Laak, R Kuehne, W. Schunack

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

A new class of histamine analogues characterized by a 3,3-diphenylpropyl substituent at the 2-position of the imidazole nucleus has been prepared outgoing from 4,4-diphenylbutyronitrile (4b) via cyclization of the corresponding methyl imidate 5b with 2-oxo-4-phthalimido-1-butyl acetate or 2-oxo-1,4-butandiol in liquid ammonia, followed by standard reactions. The title compounds displayed partial agonism on contractile H
Original languageEnglish
Pages (from-to)1071-1084
JournalJournal of Medicinal Chemistry
Volume43
Issue number6
DOIs
Publication statusPublished - 2000

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