Synthesis and antihistaminic activity of some thiazolidin-4-ones.
A new series of 2-(4- and 3-substituted phenyl)-3-[3-(N,N-dimethylamino) propyl]-1,3-thiazolidin-4-ones were synthesized, characterized, and evaluated for their ability to inhibit the contractions induced by histamine on guinea pig ileum. The measurement of pA2 values suggested that the reported compounds showed H1-antagonism. The more active compounds 5, 9, and 13 exhibited activity close to that of mepyramine.
Università di Napoli Federico II, Facoltà di Farmacia, Italy.
M V
MV
Diurno
O
O
Mazzoni
E
E
Piscopo
A
A
Calignano
F
F
Giordano
A
A
Bolognese
D000818:Animals; D005260:Female; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014961:X-Ray Diffraction
D006634:Histamine H1 Antagonists; D013844:Thiazoles