Synthesis and biological evaluation of some new heterocyclesincorporating pyrazole ring / Nany Salah Eldin Serag ; Supervised Magda A. Abdallah , Sobhi M. Gomha , Mohamed R. Abdelaziz

Thesis (M.Sc.) - Cairo University - Faculty of Science - Department of Organic Chemistry

The original work of the submitted thesis consists of three research projects: The first project: A series of novel thiazoles and 1, 3-thiazine derivatives were synthesized in a good yield via reaction of ethyl 3-(1-(2-thiocarbamoylhydrazono) ethyl)-1, 5-diphenyl- 1H-pyrazole-4-carboxylate with hydrazonoyl halides and arylidenemalononitriles, respectively. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data and alternative routes whenever possible. Moreover, the antiviral screening of the products was evaluated and the results revealed that some of them have high to moderate potency against rabies virus compared with the reference drug. The second project: Ethyl 3-acetyl-1, 5-diphenyl-1H-pyrazole-4-carboxylate reacts with a variety of arylaldehydes by grinding method in the presence of catalytic amount of sodium hydroxide at ambient temperature to give the respective chalcones. The latter compounds react also by grinding method with nitrogen nucleopliles such as hydrazine hydrate, phenylhydrazine and thiosemicarbazide to afford the corresponding pyrazol-3-yl pyrazoles. A series of 6-pyrazolylpyrimidine-2-thione derivatives were prepared by reaction of the above chalcones with thiourea by grinding method in the presence of catalytic amount of sodium hydroxide at room temperature. Also, 7-pyrazolylpyridopyrimidine-3-thione was also prepared by reaction of chalcone with 6-aminothiouracil. All the newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR, 1H and 13C NMR, Mass). Moreover, some of the products were evaluated for their antiviral activity against Herps virus, at different concentrations. The results obtained indicated that some of the products have promising activity

Issued also as CD