Premium
Design and development of some thiazole‐based flavanoids as novel antibacterial against pathogens causing surgical site infection for possible benefit in bone trauma via inhibition of DNA gyrase
Author(s) -
Zhao Gang,
Lan Dengzhe,
Qi Guobao
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12999
Subject(s) - dna gyrase , thiazole , antibacterial activity , staphylococcus aureus , chemistry , enzyme , dna , antibiotics , stereochemistry , biochemistry , bacteria , combinatorial chemistry , microbiology and biotechnology , escherichia coli , biology , gene , genetics
In this study, a novel class of hybrid thiazole‐based flavanoid derivatives were synthesized and characterized by FT ‐ IR , 1 H‐ NMR , 13 C‐ NMR , mass and elemental analysis. These derivatives were evaluated for antibacterial activity for possible benefit in bone trauma via inhibition of DNA gyrase enzyme. Results suggested that compounds 9n , 9o , and 9p showed considerable inhibition of DNA gyrase with considerable activity against tested forty strains of Staphylococcus aureus clinical isolates. Moreover, compound 9n showed hydrogen bonding with LYS 460 along with low binding free energy of −4.36 kcal/mol against DNA gyrase enzyme. The hemolytic activity of the potent compounds showed mild to no activity together with excellent pharmacokinetics, suggesting to have a potential for the development of designed compounds as novel antibacterial agents.