Histamine H-1 receptor ligands Part I. Novel thiazol-4-ylethanamine derivatives: synthesis and in vitro pharmacology

Citation
K. Walczynski et al., Histamine H-1 receptor ligands Part I. Novel thiazol-4-ylethanamine derivatives: synthesis and in vitro pharmacology, FARMACO, 54(8), 1999, pp. 533-541
Citations number
28
Categorie Soggetti
Pharmacology & Toxicology
Journal title
FARMACO
ISSN journal
0014827X → ACNP
Volume
54
Issue
8
Year of publication
1999
Pages
533 - 541
Database
ISI
SICI code
0014-827X(19990830)54:8<533:HHRLPI>2.0.ZU;2-7
Abstract
A series of 2-substituted thiazol-4-ylethanamines have been synthesized and tested for their histaminergic H-1-receptor activities. The compounds with 2-phenyl substitution, regardless of the different physicochemical propert ies of the meta-substituents at the phenyl ring, showed weak H-1-agonistic activity with pD(2) values ranging from 4.35 to 5.36. When the phenyl group was replaced by a benzyl group, the resulting compounds all exhibited weak H-1-antagonistic activity (pA(2): 4.14-4.82). (C) 1999 Elsevier Science S. A. All rights reserved.