Ahmed F. El-Farargy

A Novel Synthesis of Some New Pyrimidine and Thiazolopyrimidine Derivatives for Anticancer Evaluation

Diaryl-oxiran-2-yl methanones ( 2 ) were prepared and reacted with thiourea to give 2-thioxo-tetrahydro-pyrimidine-5(2H)-ones ( 3 ).The latter compounds reacted with bromoacetic acid to afford the title compounds ( 4 ). Also some new derivatives were prepared from the reaction of compounds ( 3 ) and ( 4 ) with different reagents. Compounds ( 3 ) were glycosidated with 2,3,4,6-tetra-O-acetyl-α -D-glucopyranosylbromide (α -ABG) to afford the corresponding nucleosides.

Synthesis and antimicrobial activities of new s-nucleosides of chromeno[2,3-B]pyridine derivatives and C-nucleosides of [1,2,4]triazolo[1,5-a]quinoline derivatives.

Direct preparation of 2-amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7,7-dimethyl-5-oxo-4H-chromene-3-carbonitrile 2 and 1,2-diamino-1,4,5,6,7,8-hexahydro-4-(4-methoxyphenyl)-7,7-dimethyl-5-oxo-3-quinolinecarbonitrile 11, which were utilized as starting products for the synthesis of S-nucleoside analogues 10 and 15 and C-nucleoside analogues 12 and 13, is presented in the current study. The antibacterial and antifungal activities of these new compounds were evaluated. The structures of the new products were confirmed on the basis of elemental and spectral analysis results.

Synthesis of Some Novel Fused Heterocyclic Compounds Derivatives from Bis-chalcones

A chalcone was prepared by the reaction of 1,4-diacetylbenzene with benzaldehyde. Reaction of this chalcone with cynanothioacetamide/guanidine hydrochloride and malnonitrile in presence of piperdene afforded the corresponding pyridine, pyrimidine, and pyrans derivatives in good yields respectively. Further, bis-chalcone 1 was cyclized to pyrazole analogs by using thiosemicarbazide, semicarbazide and tertiarybutylcarbazate. The newly heterocyclic compounds have been characterized by IR, 1H-NMR and elemental analyses.