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
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.