期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 40, 期 1, 页码 15-23出版社
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2004.09.010
关键词
histamine H-3-receptor; H-3-antagonists; 1-[(2-thiazolopyridine)-4-n-propyl]piperazines; 1[(2-oxazolopyridine)-4-n-propyl]piperazines; 1-[(2-benzothiazole)-4-n-propyl]piperazine; 1-[(2-benzothiazole)-4-n-propyl]piperazine
In search for a new lead of non-imidazole histamine H-3-receptor antagonists, a series of 1[(2-thiazolopyridine)-4-n-propyl]piperazines, the analogous 1-[(2-oxazolopyridine)-4-npropyl]piperazines, 1-[(2-benzothiazole)-4-n-propyl]piperazine and 1-[(2-benzooxazole)4-n-propyl]piperazine were prepared and in vitro tested as H-3-receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). It appeared that by comparison of homologous pairs the thiazolo derivatives have slightly higher activity than their oxazolo analogues. The most potent compound of these series is the 1-(2-thiazolo[4,5-c]pyridine)-4-n-propylpiperazine (3c) with pA(2) = 7.25 (its oxazole analogue (4g) showed pA(2) = 6.9). The structure-activity relationships for compounds with various positions of the nitrogen in the benzene ring for the thiazoles compared with oxazoles are discussed. (C) 2004 Elsevier SAS. All rights reserved.
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