SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVE: DERIVED FROM CIPROFLOXACIN

  • ANUJ SINGHAI Department of Pharmaceutical Chemistry, Oriental College of Pharmacy and Research, Oriental University, Indore, Madhya Pradesh, India.
  • GUPTA MK Department of Pharmacognosy, Oriental College of Pharmacy and Research, Oriental University, Indore, Madhya Pradesh, India.

Abstract

Objective: The purpose of this research is synthesized and evaluates different derivatives of oxadiazole.


Methods: A novel series of substituted 1,3,4-oxadiazole derivative were synthesized by condensing different amine with 1-cyclopropyl-6-fluoro-7- (piperazin-1-yl)-3-(5-thioxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)quinolin-4(1H)-one (III) in the presence of formaldehyde. The structure of these novel synthesized compounds was characterized on the bases of physicochemical and spectral analysis. The title compounds (IVa-h) were screened for antibacterial activity by disc diffusion method.


Results: Substituted 1,3,4-oxadiazole derivative was synthesized, characterized, and evaluated for antibacterial activity. Compounds IVa, IVd, IVe, IVf, and IV h showed enhance activities then ciprofloxacin against all Gram-positive and Gram-negative organisms. Compound IVe showed the highest activity against Staphylococcus aureus and compound IV showed the highest activity against Escherichia coli.


Conclusion: The present study demonstrates the synthesis and characterization of 1,3,4-oxadiazole derivatives derived from ciprofloxacin. These compounds were evaluated for antibacterial activity against different Gram-positive and Gram-negative organism. In some cases, antibacterial activity is found to be enhanced as compared to standard drug ciprofloxacin.

Keywords: 1,3,4-Oxadiazole, Ciprofloxacin, Antimicrobial

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ANUJ SINGHAI, and GUPTA MK. “SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF SUBSTITUTED 1,3,4-OXADIAZOLE DERIVATIVE: DERIVED FROM CIPROFLOXACIN”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 12, no. 9, July 2019, pp. 205-9, https://innovareacademics.in/journals/index.php/ajpcr/article/view/34712.
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