A convenient and efficient three-component reaction to a one-pot synthesis of thiophene derivatives from activated acetylenic compounds and ethyl 2chloroacetoacetate in the presence of tetramethyl thiourea in water lead to the formation of thiophenes in good yields.

Thiourea derivatives demonstrate potent cytotoxic activity against various leukemias and many tumor cell lines. In our previous study, the combination of thiourea and phosphonate has been proven as an effective strategy for developing antitumor agents. Herein, we synthesized and evaluated a series of novel chiral dipeptide thioureas containing an α-aminophosphonate moiety as antitumor agents. F...

For the first time, chiral sulfoximine derivatives have been applied as asymmetric organocatalysts. In combination with a thiourea-type backbone the sulfonimidoyl moiety leads to organocatalysts showing good reactivity in the catalytic desymmetrization of a cyclic meso-anhydride and moderate enantioselectivity in the catalytic asymmetric Biginelli reaction. Straightforward synthetic routes prov...

The recent discovery of the rodenticidal properties of a-naphthylthiourea (ANTU) by Richter (1) has aroused interest in the mechanism by which this compound produces its acute toxic effects in animals. Factors associated with the toxicity of ANTU such as (a) the high toxicity to Norway rats, (b) the lower toxicity to most other species, (c) the development of tolerance after administration of s...

The recent discovery of the rodenticidal properties of a-naphthylthiourea (ANTU) by Richter (1) has aroused interest in the mechanism by which this compound produces its acute toxic effects in animals. Factors associated with the toxicity of ANTU such as (a) the high toxicity to Norway rats, (b) the lower toxicity to most other species, (c) the development of tolerance after administration of s...

The synthesis and biological evaluation of new types of N,N′-disubstituted thiourea and urea derivatives as inhibitors of both neuronal nitric oxide synthase (nNOS) and inducible nitric oxide synthase (iNOS) are described. These compounds have been designed by reduction of the carbonyl group in the thiourea and urea kynurenamine derivatives 3 previously synthesized by our research group. The sy...

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 methodology offers se...