Synthesis and biological activities of some thiazolidin-4-ones.
In this study, fifteen 2,3-disubstituted-4-thiazolidinone derivatives were synthesized by the reaction of Schiff bases and alpha-mercaptoacetic acid. The structures of the compounds were elucidated by IR, 1H-NMR, 13C-NMR, mass spectral data and elementary analysis. The antihistaminic and anticholinergic activities of the compounds were determined by tests performed on isolated guinea pig trachea in comparison with aminophylline (CAS 317-34-0). Compound 15 (3-[3-(2-methyl-piperidine-1-yl)propyl]-2-(4-methyl-phenyl)thiazolidin-4-one hydrochloride) showed the highest inhibition (53 %).
Ozadali
Keriman
K
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Ozkannli
Fügen
F
Erol
Dilek
D
Doğan
Ali Evrim
AE
Erol
Kevser
K
D000109:Acetylcholine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000818:Animals; D018680:Cholinergic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D009119:Muscle Contraction / Q000187:drug effects; D012545:Schiff Bases / Q000138:chemical synthesis / Q000494:pharmacology; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014132:Trachea / Q000187:drug effects; D014665:Vasodilator Agents / Q000037:antagonists & inhibitors / Q000494:pharmacology
D018680:Cholinergic Antagonists; D006633:Histamine Antagonists; D007202:Indicators and Reagents; D012545:Schiff Bases; D053778:Thiazolidines; D014665:Vasodilator Agents; D000109:Acetylcholine