Histamine H1 receptor ligands Part I.: Novel thiazol-4-ylethanamine derivatives:: synthesis and in vitro pharmacology

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 properties 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.