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Histamine H 1 receptor ligands: Part II. Synthesis and in vitro pharmacology of 2-[2-(phenylamino) thiazol-4-yl] ethanamine and 2-(2-benzhydrylthiazol-4-yl) …

K Walczyński, R Guryn, OP Zuiderveld, MQ Zhang…

Index: Walczynski, Krzysztof; Guryn, Roman; Zuiderveld, Obbe P.; Zhang, Ming-Qiang; Timmerman, Henk Farmaco, 2000 , vol. 55, # 9-10 p. 569 - 574

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Citation Number: 16

Abstract

New 2-[2-(phenylamino) thiazol-4-yl] ethanamine and 2-(2-benzhydrylthiazol-4-yl) ethanamine derivatives were prepared and tested in vitro as H1 receptor antagonists. The compounds with 2-phenylamino substitution with meta-halide substituents at the phenyl ring, showed weak H1-antagonistic activity (pA2: 4.62–5.04) and this activity was completely lost in the case of meta-methyl substituent (pA2< 4). When the phenylamino group was ...