title: Histamine H1 receptor ligands: part II. Synthesis and in vitro pharmacology of 2-[2-(phenylamino)thiazol-4-yl]ethanamine and 2-(2-benzhydrylthiazol-4-yl)ethanamine derivatives.
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 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).
authors.affiliation: Department of Synthesis and Technology of Drugs, Medical Academy, Lódz, Poland.
authors.forename: K
authors.initials: K
authors.lastname: Walczyński
authors.forename: R
authors.initials: R
authors.lastname: Guryn
authors.forename: O P
authors.initials: OP
authors.lastname: Zuiderveld
authors.forename: M Q
authors.initials: MQ
authors.lastname: Zhang
authors.forename: H
authors.initials: H
authors.lastname: Timmerman
mesh_terms: D000818:Animals; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D015394:Molecular Structure; D011969:Receptors, Histamine H1 / Q000378:metabolism*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D005021:Ethylamines; D006633:Histamine Antagonists; D008024:Ligands; D011969:Receptors, Histamine H1; D013844:Thiazoles