الفهرس | Only 14 pages are availabe for public view |
Abstract A series of pyrimdine and thiazine derivatives synthesized by one pot reaction of cyclopentanone with a mixture of an aromatic aldehyde namely o-anisaldehyde and different ureas namely urea, guandine and thiourea respectively. Furthermore, cycloaddition reaction of active methylene reagents namely acetyl acetone, malononitrile, ethyl cyanoacetate, cyanoacetamide and N-phenyl cyanoacetamide with 2,6-bis(2-methoxybenzylide)-cyclohexanone afforded chromene and quinoline derivatives in basic medium. The antitumor evalution of some new compounds against three human cell lines namely MCF-7, NCI-H460 and SF-268 showed significant and moderate activity compared with positive control doxorubicin. In this study, a convenient synthetic methods for novel heterocyclic products like pyrimidin-2(1H)-one, pyrimidine-2(1H)-thione, pyrimido[1,2-a]pyrimidine, pyrazole, pyran-3-carbonitrile, 2-oxo-1,2-dihydropyridine, 3-cyanopyridin-2-yl malononitrile, pyrido[2,3-d]pyrimidinedione, chromeno[3,4-c]pyridinedione and pyrano[3,4-c]chromen-5-one derivatives were successfully developed by reacting a α,β-unsaturated ketone with 1,2; 1,3-bidentate nitrogen and carbon nucleophiles. Furthermore, the newly synthesized compounds were screened for their antimicrobial activity against Staphylococcus aureus, Bacillis subtilis, Escherichia coli and Aspergillus flavus and were compared with standard drugs. Most of the tested compounds exhibited promising activity. An efficient for the preparation of novel pyrimidinthione 56 from [3+3] cycloaddition hydrazone 55 and benzoylisothiocyanate. Compound 55 was added to carbon disulphide to furnish 57. Hydrazide derivative 54 underwent condensation reaction with chalcone and / or diethyl butylmalonate to produce oxadiazebine 60 and/or 61 respectively. |