Histamine H1 receptor ligands
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Add time:07/12/2019 Source:sciencedirect.com
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 replaced by benzhydryl groups of classic antihistamines, the resulting compounds exhibited slightly improved H1-antagonistic activity (at the meta-position pA2: 6.38–6.15; at the para-position pA2: 6.04–5.87).
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