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Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H-3-receptor antagonists

Stark, H; Ligneau, X; Sadek, B; Ganellin, CR; Arrang, JM; Schwartz, JC; Schunack, W; (2000) Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H-3-receptor antagonists. Bioorganic and Medicinal Chemistry Letters , 10 (20) 2379 - 2382.

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Abstract

Novel derivatives of the highly potent and selective histamine H-3-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. (C) 2000 Elsevier Science Ltd. All rights reserved

Type:Article
Title:Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H-3-receptor antagonists
Additional information:Journal Article OCT 16 365MV Stark H Free Univ Berlin, Inst Pharm, Konigin Luise Str 2&4, D-14195 Berlin, Germany BIOORG MEDICINAL CHEM LETTER
Keywords:antagonist, ANTAGONISTS, As, ciproxifan, DERIVATIVES, H-3 receptor, H-3-RECEPTOR ANTAGONIST, HIGHLY POTENT, Histamine, in vitro, in vivo, In-vitro, in-vivo, LENGTH, letter, novel, Oral, Other, POTENT, RANGE, Science, VARIANT, VARIANTS
UCL classification:UCL > School of BEAMS > Faculty of Maths and Physical Sciences > Chemistry

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