Design, synthesis, antimicrobial activity and molecular modeling studies of novel benzofuroxan derivatives against Staphylococcus aureus.

摘要: Molecular modification is a quite promising strategy in the design and development of drug analogs with better bioavailability, higher intrinsic activity less toxicity. In search new leads potential antimicrobial activity, series 14 4-substituted [N'-(benzofuroxan-5-yl)methylene]benzohydrazides, nifuroxazide derivatives, were synthesized tested against standard multidrug-resistant Staphylococcus aureus strains. The selection substituent groups was based on physicochemical properties, such as hydrophobicity electronic effect. These properties also evaluated through lipophilic electrostatic maps, respectively, considering compounds biological profile. Twelve exhibited similar bacteriostatic most active compound 4-CF(3) substituted derivative, which presented minimum inhibitory concentration (MIC) value 14.6-13.1 microg/mL, ClogP 1.87. results highlight benzofuroxan derivatives for designing future candidates.