Influence of bulky substituents on histamine H3 receptor agonist/antagonist properties

A Sasse, X Ligneau, A Rouleau, S Elz…

Index: Sasse, Astrid; Ligneau, Xavier; Rouleau, Agnes; Elz, Sigurd; Ganellin, C. Robin; Arrang, Jean-Michel; Schwartz, Jean-Charles; Schunack, Walter; Stark, Holger Journal of Medicinal Chemistry, 2002 , vol. 45, # 18 p. 4000 - 4010

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Citation Number: 22

Abstract

Novel derivatives of 3-(1 H-imidazol-4-yl) propanol were designed on the basis of lead compounds belonging to the carbamate or ether series possessing (partial) agonist properties on screening assays of the histamine H3 receptor. One pair of enantiomers in the series of α-methyl-branched chiral carbamates was stereoselectively prepared in high optical yields. Enantiomeric purity was checked by Mosher amide derivatives of ...