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Synthesis and structure-activity relationships of 2-(substituted phenyl)-3-[3-(N,N-dimethylamino)propyl]-1,3-thiazolidin-4-ones acting as H1-histamine antagonists.
- Source :
-
Farmaco (Societa chimica italiana : 1989) [Farmaco] 1999 Sep 30; Vol. 54 (9), pp. 579-83. - Publication Year :
- 1999
-
Abstract
- 2-(Substituted-phenyl)-3-[3-(N,N-dimethylamino)propyl]-1,3-thiazolidi n-4- ones (1-15) showed dependence of the potency of the H1-histamine antagonism on the m- and p-substituents suggesting that the aromatic moiety binds the receptor by a strong pi-interaction. Electron-withdrawing substituents decrease the potency while the electron-donating alkyl substituents, enhancing the aryl HOMO energy, increase the antihistamine activity. The m-substituents with the capability to form hydrogen bonds, seems to share an extra-interaction with hydrogen accepting or donating groups of the histamine receptor and exhibits very high potency.
Details
- Language :
- English
- ISSN :
- 0014-827X
- Volume :
- 54
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Farmaco (Societa chimica italiana : 1989)
- Publication Type :
- Academic Journal
- Accession number :
- 10555258
- Full Text :
- https://doi.org/10.1016/s0014-827x(99)00064-6