Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)-and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine.

I.J.P. de Esch, R.C. Vollinga, K. Goubitz, H. Schenk, U. Appelberg, U. Hacksel, S. Lemstra, M. Hoffmann, R. Leurs, W.M.P.B. Menge, H. Timmerman, O.P. Zuiderveld

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Abstract

Various approaches to the synthesis of all four stereoisomers of 2-(1H- imidazol-4-yl)cyclopropylamine (cyclopropylhistamine) are described. The rapid and convenient synthesis and resolution of trans-cyclopropylhistamine is reported. The absolute configuration of its enantiomers was determined by single-crystal X-ray crystallographic analysis. The distinct transcyclopropylhistamine enantiomers were tested for their activity and affinity on the histamine H
Original languageEnglish
Pages (from-to)1115-1122
JournalJournal of Medicinal Chemistry
Volume43
DOIs
Publication statusPublished - 1999

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