NEW POTENT HISTAMINE H-3 RECEPTOR ANTAGONISTS OF THE AMIDE TYPE

被引：12
|
作者：
STARK, H
LIPP, R
ARRANG, JM
GARBARG, M
LIGNEAU, X
SCHWARTZ, JC
SCHUNACK, W
机构：
[1] FREE UNIV BERLIN, INST PHARM, D-14195 BERLIN, GERMANY
[2] LAB BIOPROJET, PARIS, FRANCE
[3] INSERM, CTR PAUL BROCA, UNITE NEUROBIOL & PHARMACOL, PARIS, FRANCE
来源：
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 1995年 / 3卷 / 02期
关键词：
HISTAMINE H-3 RECEPTOR; ANTAGONIST; IMIDAZOLYLALKYL AMIDE; POTENCY; SELECTIVITY; DRUG DEVELOPMENT;
D O I：
10.1016/0928-0987(94)00079-F
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A new class of histamine H-3-receptor antagonists is described. Structure-activity relationships of amides show essential and non-essential, but affinity increasing structural requirements by example of 27 different imidazole derivatives. The most potent compound in this series is 3-cyclopentyl-N-[3-(1H-imidazol-4-yl)propyl]propanamide (18, -log K-i = 8.3) which is equipotent to the reference antagonist thioperamide (Arrang et al., 1987) and shows high selectivity to the histamine H-3-receptor. New amides with different chain length and different lipophilic moieties are investigated. A number of compounds are similarly potent as compound 18. Structural requirements of antagonists interacting with the H-3-receptor are discussed. In general, these new amides of the imidazolylalkyl type are potent and selective histamine H-3-receptor antagonists.
引用
收藏
页码：95 / 104
页数：10
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