315674-93-2Relevant academic research and scientific papers
Convenient procedures for synthesis of ciproxifan, a histamine H3-receptor antagonist
Stark, Holger
, p. 315 - 316 (2007/10/03)
Cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl methanone (ciproxifan) is a novel reference antagonist for the histamine H3 receptor. Despite the former Mitsunobu reaction the actual key reaction for preparation based on S(N)Ar for acylated fluoroaromatics with an additional cyclization in a one-pot procedure needs no chromatographic purification steps and results in good yields.
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists
Stark, Holger,Ligneau, Xavier,Sadek, Bassem,Ganellin,Arrang, Jean-Michel,Schwartz, Jean-Charles,Schunack, Walter
, p. 2379 - 2382 (2007/10/03)
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. (C) 2000 Elsevier Science Ltd.
Novel histamine H3-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds
Stark,Sadek,Krause,Huls,Ligneau,Ganellin,Arrang,Schwartz,Schunack
, p. 3987 - 3994 (2007/10/03)
Novel histamine H3-receptor antagonists possessing a 4-(3-(phenoxy)propyl)-1H-imidazole structure generally substituted in the para-position of the phenyl ring have been synthesized according to Mitsunobu or S(N)Ar reactions. With in vitro and
