Novel approach for synthesis of potent antimicrobial hybrid molecules containing pyrimidine-based imidazole scaffolds

作者：Desai N C^*; Vaghani H V; Rajpara K M; Joshi V V; Satodiya H M

来源：Medicinal Chemistry Research, 2014, 23(10): 4395-4403.

DOI：10.1007/s00044-014-1005-1

• Pyrimidine
• Imidazole
• Antimicrobial activity
• MIC
• Hybrid molecules

This report describes the novel approach for the synthesis and exploration of hybrid molecules containing pyrimidine-based imidazole scaffolds as potent antimicrobial agents. The targeted compounds N-(4-arylidene-2-mercapto-5-oxo-4,5-dihydro-1H-imidazol-1-yl)-6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxamides (5a-l) were achieved by the Knoevenagel condensation of a key precursor (4) with different aldehydes in good yields having moderate to excellent antimicrobial activity. The structural identification of final products was carried out by known classical spectral techniques like IR, H-1 NMR, C-13 NMR, and mass spectra. The obtained data indicated that the majority of the tested compounds exhibited good antibacterial activity over antifungal activity, particularly compounds 5j and 5b (having MIC values 12.5 mu g/mL) showed a comparable effect to a standard antibacterial and antifungal agents.

• 出版日期2014-10
• 单位SAP