Back to Search
Start Over
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.
- Source :
-
Farmaco (Societa chimica italiana : 1989) [Farmaco] 2000 Sep-Oct; Vol. 55 (9-10), pp. 569-74. - Publication Year :
- 2000
-
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).
- Subjects :
- Animals
Ethylamines chemical synthesis
Ethylamines chemistry
Guinea Pigs
Histamine Antagonists chemical synthesis
Histamine Antagonists chemistry
Ligands
Male
Molecular Structure
Thiazoles chemical synthesis
Thiazoles chemistry
Ethylamines pharmacology
Histamine Antagonists pharmacology
Receptors, Histamine H1 metabolism
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0014-827X
- Volume :
- 55
- Issue :
- 9-10
- Database :
- MEDLINE
- Journal :
- Farmaco (Societa chimica italiana : 1989)
- Publication Type :
- Academic Journal
- Accession number :
- 11152236
- Full Text :
- https://doi.org/10.1016/s0014-827x(00)00087-2