Synthesis and biological evaluation of a new class of quinazolinone azoles as potential antimicrobial agents and their interactions with calf thymus DNA and human serum albumin. Issue 1 (31st October 2014)

• Record Type: Journal Article
• Authors: Peng, Li-Ping; Nagarajan, Sangaraiah; Rasheed, Syed; Zhou, Cheng-He
• Is Part Of: MedChemComm. Volume 6:Issue 1(2015:Jan.)
• Page Start: 222
• Page End: 229
• Publication Date: 2014-10-31
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c4md00281d
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : A series of quinazolinone azoles were synthesized and screened for their antimicrobial activities, and further studies of their binding behaviors with calf thymus DNA and human serum albumin were investigated. Abstract : A series of novel quinazolinone azoles were synthesized and characterized by NMR, IR, MS and HRMS spectra. Bioactive assays showed that some target compounds exhibited significant antimicrobial potency. Especially, nitroimidazole derivative3a displayed comparable or even superior antibacterial efficacies (MIC = 0.03–0.05 μmol mL −1 ) in contrast with norfloxacin (MIC = 0.01–0.05 μmol mL −1 ) and chloromycin (MIC = 0.02–0.10 μmol mL −1 ). The preliminary interactive investigations of compound3a with calf thymus DNA by UV-vis spectroscopy revealed that compound3a could bind to DNA to form compound3a –DNA complex by an intercalative mode and further block DNA replication to exert powerful antibacterial and antifungal activities. Hydrogen bonds and van der Waals forces played important roles in the association of compound3a –HSA.