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ID: ALA1132788
Journal: Bioorg Med Chem Lett
Title: Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
Authors: Stark H, Ligneau X, Sadek B, Ganellin CR, Arrang JM, Schwartz JC, Schunack W.
Abstract: Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose.
CiteXplore: 11055360