Selective S1P(1) receptor agonists have therapeutic potential to treat a variety of immune-mediated diseases. A series of 2-imino-thiazolidin-4-one derivatives displaying potent S1P(1) receptor agonistic activity were selected to establish 3D-QSAR models using CoMFA and CoMSIA methods. Internal and external cross-validation techniques were investigated as well as some measures including region ...

In this work we present the results of a study of the X-ray structure of 2-[(2,4-dimethoxyphenyl)amino]-1,3-thiazolidin-4-one. Using the FTIR spectra in solid state and results of ab initio calculations we explain the issue of the tautomerism of this molecule. The compound is shown to exist as the 2-amino tautomer rather 2-imino tautomer. Here we consider eight possible tautomers. On the basis ...

Novel 2-arylthiazolidin-4-one derivatives (8a-q and 11) have been synthesized in good-to-excellent yields (70-96%) by one-pot three-component condensation-cyclization reaction of aromatic or aliphatic primary amines, aromatic aldehydes, and thioglycolic acid in polypropylene glycol at 110°C temperature. The in vitro antimicrobial activity of the synthesized 2-arylthiazolidin-4-ones was investig...

Thiazolidine-4-one substituted 1, 2, 4triazole and benzofuran heterocyclic have received considerable attention during last two decades as they are endowed with variety of biological activities and have wide range of therapeutic properties. A literature survey indicates that benzofuran derivatives possess different pharmacological and biological activities, of which the most potent is anti-micr...

Some [(5Z)-(5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)]acetic acids were prepared as potential antifungal compounds. The general synthetic approach to all synthesized compounds is presented. Lipophilicity of all the discussed rhodanine-3-acetic acid derivatives was analyzed using a reversed phase high performance liquid chromatography (RP-HPLC) method. The procedure was performed und...

For the discovery of new antimicrobial drugs, derivatives sulfonamide having thiazole ring were synthesized. The series synthesized starting from 4-(arylsulfonamido)-acetophenone thiosemicarbazones 2a–f. Cyclization thiosemicarbazone 2a–f by using ethyl chloroacetate and chloroacetone gave thiazolidin-4-ones 3a–f 4-methylthiazoles 4a–e, respectively. properties compounds investigated. major no ...

Four imines, the condensation products of 2,4-dioxo-4-phenylbutanal with four primary amines, were condensed with mercapto acetic acid to obtain thiazolidinon-4-ones which on subsequent condensation with vanillin and isatin separately yielded eight thiazolidin-4-one derivatives. The chemical structures of the synthesized compounds were elucidated by elemental analysis, molecular weight determin...

A series of thiazolidin-4-one (2a–h; 3a–h), azetidin-2-one (4a–h) and 1,3,4-oxadiazole (5a–h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. The structures of the new compounds were supported by their IR, 1H-NMR and mass spectral data. All compounds w...