रासायनिक अनुसंधान में पुरालेख खुला एक्सेस

अमूर्त

Synthesis and in vitro Anticancer and Antimicrobial Evaluation of Novel Substituted Dihydropyrimidines

Kulbhushan  Rana

Background: Anticancer drug discovery and development is one of the most essential and rapidly changing avenues for medicinal chemist. The requirement for new chemotherapeutics in cancer is evident due to the limited capacity of drugs to cure or significantly prolong the survival of patients with disseminated tumours or certain leukemias. Despite large number of antibiotics and chemotherapy available for medicinal use, the treatment of infectious diseases still remains an important and challenging problem.

Objective: To synthesize new dihydropyrimidine derivatives and check their anticancer, antibacterial and antifungal activities.

Methods: A series of 1,4-dihydropyrimidine derivatives were prepared from Biginelli reactions by using ethyl acetoacetate, substituted benzaldehyde and thiourea in the presence of piperidine and ethanol. The compounds were reacted with dimethylsulphate, diethylsulphate, butyl bromide and benzyl chloride to give the new series of compounds. The structures of the newly synthesized compounds were established by IR, ¹H NMR, Mass spectra and elemental analysis. The synthesized compounds were evaluated for theirin-vitro anticancer activity by using SRB assay method against the growth of four human’s cancer cell lines, antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli and for antifungal activity against Candida albicans and Aspergillus niger.