We report a series of 4-sulfamoylphenyl-ω-aminoalkyl ethers as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The structure-activity relationship was drawn for the inhibition of four physiologically relevant isoforms: hCA I, II, IX, and XII. Many of these compounds were highly effective, low nanomolar inhibitors of all CA isoforms, whereas several isoform-selective were also identified. X-ray ...

The synthesis of four symmetrical compounds containing urea/thiourea and anthracene/nitrobenzene groups was optimized. N,N'-Di((anthracen-9-yl)-methylene) thio-carbonohydrazide showed sensitive and selective binding ability for acetate ion among the studied anions. The presence of other competitive anions including F(-), H₂PO₄(-), Cl(-), Br(-) and I(-) did not interfere with the strong binding ...

A diastereo- and enantio-selective domino Michael-cyclization-tautomerization reaction of isatylidene malononitriles with α,α-dicyanoalkenes catalyzed by a cinchona alkaloid-derived bifunctional thiourea catalyst has been developed. A series of multi-functionalized spiro oxindole diene derivatives have been obtained in good to excellent yields (up to 97%) with good to excellent enantioselectivi...

A family of 9-amino(9-deoxy) epicinchonine derivatives, possessing a range of mono- and bidentate hydrogen bond donor groups at the 9-position, were synthesised and evaluated for asymmetric organocatalytic activity in the dimethyl malonate Michael addition to beta-nitrostyrene; thiourea derivative was identified as the most effective bifunctional organic catalyst and found to induce high enanti...

The new novel series of 2-amino-5-phenyl thiazole derivatives were occurred in the reaction between thiourea and various substituted ketones. The reactions were carried out in the microwave oven under solvent free condition. The completion of the reactions was checked by TLC. The structures of the compounds were characterized by FT-IR, 1 H and 13 C NMR and elemental analysis. Synthesized compou...

The unprecedented diaza-ene reaction of formaldehyde N-tert-butyl hydrazone with nitroalkenes can be efficiently catalyzed by an axially chiral bis-thiourea to afford the corresponding diazenes in good to excellent yields (60-96%) and moderate enantioselectivities, up to 84 : 16 er; additional transformation of diazenes into their tautomeric hydrazones proved to be operationally simple and high...

The effects of thiourea injection on scale development were studied in New Hampshire Red x White Leghorn Cross chick embryos. Normal morphogenesis and keratinization of scales were significantly delayed in thioureatreated specimens. Subsequent thyroxine injection resulted in normal or even precocious scale development. The thyroid hormone responsiveness of scale development is discussed in rela...

A series of 2,5,7-trisubstituted pyrimido[4,5-d]pyrimidine cyclin-dependent kinase (CDK2) inhibitors is designed and synthesized. 6-Amino-2-thiouracil is reacted with an aldehyde and thiourea to prepare the pyrimido[4,5-d]-pyrimidines. Alkylation and amination of the latter ones give different amino derivatives. These compounds show potent and selective CDK inhibitory activities and inhibit in ...

Nowadays, the Human Immunodeficiency Virus (HIV), which is the causative agent of Acquired Immune Deficiency Syndrome (AIDS), represents a serious public health problem. According to the World Health Organization (WHO), in 2009 there were 33.3 million people living with HIV worldwide, and more particularly in sub-Saharan Africa, where the overwhelming majority (67%) of cases appear. Furthermore...