In this work the structural requirements of both urea and thiourea derivatives were evaluated for optimal antibacterial activity on Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli, using several organic compounds (VI-X) as chemical tools. In order to delineate the structural chemical requirements of studied compounds, the descriptors Log P, π MR and MV were calculated. The res...

Oxalic acid dihydrate as a green, mild and efficient catalyst for the one-pot three-component Biginelli synthesis of 3,4-dihydropyrimidin-2-(1H)-one derivatives from the reaction between β-keto esters (methyl or ethyl acetoacetate), aromatic aldehyde (benzaldehye derivatives) and urea or thiourea under thermal and solvent-free conditions with excellent yields and short reaction time is st...

An efficient and simple one-pot approach for the synthesis of 3,4-dihydropyrimidin-2-(1H)-one derivatives using antimony trichloride (SbCl3) as a mild catalyst by means of three-component Biginelli reaction between β-keto esters, aldehyde derivatives and urea/thiourea under thermal and solvent-free conditions with excellent yields and short reaction times is reported. This m...

Oxalic acid dihydrate as a green, mild and efficient catalyst for the one-pot three-component Biginelli synthesis of 3,4-dihydropyrimidin-2-(1H)-one derivatives from the reaction between β-keto esters (methyl or ethyl acetoacetate), aromatic aldehyde (benzaldehye derivatives) and urea or thiourea under thermal and solvent-free conditions with excellent yields and short reaction time is st...

A new class of aminocyclitol derivatives with the bicyclo[4.2.0]octane skeleton was synthesized starting from cyclooctatetraene. Photooxygenation of trans-7,8-diacetoxy- and cis-7,8-dichlorobicyclo[4.2.0]octa-2,4-diene afforded the bicyclic endoperoxides. Reduction of the latter with thiourea followed by a Pd(0) catalyzed ionization/cyclization reaction gave the corresponding oxazolidinone deri...

Synthesis and antibacterial activity of some novel urea and thiourea derivatives (7a-7k, 8a-8f) of anacardic acid prepared from commercially available anacardic acid which is obtained from natural product Cashew Nut Shell Liquid (CNSL). Compounds (7a-7k, 8a-8f) were tested for Gram positive and Gram negative bacterial cultures. Most of the compounds were showed active compared with standard dru...

A novel series of sulfonamide derivatives (14 compounds) bearing thiourea moieties were efficiently synthesized and evaluated for their possible in vitro anticancer activity against four human tumor cell lines. The results indicated that compound 6 was the most potent, showing effectiveness on all the tested cell lines. Compounds 7 and 10 also showed promising results.

A series of chalcones, dihydropyrimidinone and dihydropyrimidinethione derivatives were synthesized in good yields by Claisen Schmidt reaction of acetophenones with substituted aldehydes in the presence of sodium hydroxide in water-ethanol mixture followed by the condensation reaction of chalcones with urea and thiourea in ethanol respectively. The structures of the synthesized compounds were e...

Highly enantio- and diastereoselective organocatalytic Mannich reactions of glycine Schiff bases with N-Boc-protected imines are described. Imines were generated in situ from bench-stable alpha-amido sulfones. Catalysis mediated by a cinchona alkaloid thiourea provided optically active alpha,beta-diamino acid derivatives with up to 99% ee and near-perfect diastereoselection.