DESIGN, SYNTHESIS, IN SILICO STUDY AND PRELIMINARY
PHARMACOLOGICAL ASSESSMENT OF NEW GATIFLOXACIN
ANALOGUES HAVING THIAZOLE NUCLEUS
الباحث الأول:
Hajer A. Jawad
الباحثين الآخرين:
Noor H. Naser
Sahar A. Hussein
المجلة:
Biochemical and cellular archives journal
تاريخ النشر:
None
مختصر البحث:
ABSTRACT : Series of gatifloxacin derivatives (IVa-IVd) were synthesized by incorporation of thiazole ring (Which has
antibacterial activity) and some of its derivatives into a secondary amine of piperazine ring at C-7 position of gatifloxacin
nuc…
ABSTRACT : Series of gatifloxacin derivatives (IVa-IVd) were synthesized by incorporation of thiazole ring (Which has
antibacterial activity) and some of its derivatives into a secondary amine of piperazine ring at C-7 position of gatifloxacin
nucleus, in order to increase bulkiness at this position by that reduce the affinity toward the efflux pump of bacterial cells,
leading to reduction in bacterial resistance. By using FT-IR spectroscopy, 1H-NMR spectral and some of the physicochemical
properties, the synthesized compounds were confirmed and characterized for their chemical structures. In-vitro study was
performed to evaluate the antibacterial effect of all synthesized compounds and was revaluated by using agar- well diffusion
method (AWD). The antibacterial study was shown a topmost inhibition zone for the compounds IVa and IVb against Staphylococcus
aureus and the lowest inhibition zone for the two compounds IVc and IVd against E. coli. In silico study was performed using
Molecular Operating Environment program and showed that all synthesized compounds were give affinity toward topoisomerase
enzyme and these studies were compatible with the in vitro studies, as the compound IVb give the highest S score value.
