Synthesis and investigation antiinflammatory activity of 5- arylmethylidene-4-oxo-2-thioxotiazolidin-3-ylalcancarboxylic acids with antipyrile moiety in molecules

Abstract

It was shown, that reaction of acylation of 4-aminoantipyrine by 5-substituted thiazolidine- 3-ylalkanecarboxylic acids chlorides yielded to N-(l,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-lH-py- razole-4-il)-4-(5-arylmethylidene-4-oxo-2-thioxothiazolidine-3-yl)alkane amides. The structure of synthesized compounds was confirmed by the NMR-spectroscopy. Studying of the antiinflammatory activity of the synthesized compounds on inflammatory oedem formaline model gave the opportunity to identify highly active compounds: N-(1,5- dimethyl-3-oxo-2-phenyl-2,3-dihydro-lH-pyrazole-4-yl)-4-(5- phenylmethylidene-4-oxo-2-thioxothiazolidine-3-yl)etane amide, N-(l,5-dimethyl-3-oxo-2-phenyl-2,3- dihydro-lH-pyrazole-4-yl)-4-(5-phenylmethylidene-4-oxo-2-thioxothiazolidine-3-yl)butane amide and N-(l,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-lH-pyrazole-4-yl)-4-[5-(4-methoxyphenylmethylidene)-4- oxo-2-thioxothiazolidine-3-yl]butane amide, which are recommended for in-depth studies.