Synthesis, characterization, antimicrobial and anticancer evaluation of pyrimidines Clubbed with thiazolidinone

Mohan Verma, Prabhakar Kumar Verma

Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, India

ABSTRACT

A series of novel derivatives of pyrimidine clubbed with thiazolidinone was synthesized in good yield and characterized by physiochemical and spectral means. All the synthesized derivatives were evaluated for their antimicrobial and anticancer activity. Antimicrobial properties of the title compounds were investigated against Gram positive (Bacillus subtilis and Staphylococcus aureus) and Gram negative bacterial (Escherichia coli) as well fungal strains (Candida albicans and Aspergillus niger). The anticancer evaluation of synthesized compounds against HeLa Cervical cancer cell Line indicated that (Z)-N-(5-(4-nitrobenzylidene)-4-oxo-2-phenylthiazolidin-3-yl)-6-methyl-4-(2-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide and (Z)-N-(5-(4-(diethylamino)benzylidene)-4-oxo-2-phenylthiazolidin-3-yl)-6-methyl-4-(2-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (PT9, IC50 = 12.68μM and PT14, IC50 = 15.27μM) was the most active anticancer agent and was more potent than standard drug, Doxorubicin (IC50 =16.12μM). All newly synthesized compounds also exhibited promising results against microbial strains.

Keywords:

Pyrimidine, Thiazolidinone, Antimicrobial activity, HeLa Cancer cell line, Anti-cancer activity.