Identification of novel 2-aminothiazole conjugated nitrofuran as antitubercular and antibacterial agents

摘要: The emergence of antibiotic resistant pathogens is an ongoing main problem in the therapy bacterial infections. In order to develop promising antitubercular and antibacterial lead compounds, we designed synthesized a new series derivatives 2-aminothiazole conjugated nitrofuran with activities against both Mycobacterium tuberculosis Staphylococcus aureus. Eight compounds 12e, 12k, 12l, 12m, 18a, 18d, 18e, 18j emerged as agents. Structure-activity relationships (SARs) were discussed showed that substituted at position-3 benzene 5-nitro-N-(4-phenylthiazol-2-yl)furan-2-carboxamide exhibited superior potency. most potent compound benzamide this position, displayed minimum inhibitory concentrations (MICs) 0.27μg/mL Mtb H37Ra 1.36μg/mL S. Furthermore, 18e had no obvious cytotoxicity normal Vero cells (IC50=50.2μM). results suggest novel scaffolds aminothiazole would be class antimicrobial