Design, synthesis, antibacterial evaluation and molecular docking studies of some new quinoxaline derivatives targeting dihyropteroate synthase enzyme
Development of new antimicrobial agents is a good solution to overcome drug-resistance problems. From this perspective, new quinoxaline derivatives bearing various bioactive heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and thiazoles) were designed and synthesized. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against nine bacterial human pathogenic strains using the disc diffusion assay. In general, most of the synthesized compounds exhibited good antibacterial activities. The thiazolyl 11c displayed significant antibacterial activities against P. aeruginosa (MIC, 12.5 µg/mL vs levofloxacin 12.5 µg/mL). Molecular docking studies indicated that the synthesized compounds could occupy both p-amino benzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could act by the inhibition of bacterial DHPS enzyme. The results provide important information for the future design of more potent antibacterial agents.
Faculty of Applied Health Sciences Technology
Life Sciences, Pharmacology, Toxicology, Pharmaceutical Science
Indexed in Scopus
Indexed in Web Of Science
Antibacterial activity, Dihyropteroate synthase, Docking, Quinoxalines, Synthesis
El-Attar, Maryam A.Z.; Elbayaa, Rasha Y.; Shaaban, Omaima G.; Habib, Nargues S.; Abdel Wahab, Abeer E.; Abdelwahab, Ibrahim A.; and El-Hawash, Soad A.M., "Design, synthesis, antibacterial evaluation and molecular docking studies of some new quinoxaline derivatives targeting dihyropteroate synthase enzyme" (2018). Faculty of Applied Health Sciences Technology. 98.