QSAR Studies and Synthesis of C-5 Substituted Derivatives of Counter Fluoroquinolone Drugs

Abstract

Fluoroquinolones have attracted much attention because of their broad spectrum of activity against various bacteria, mycobacteria and parasites but there are numerous factors including solubility, side effects and cost of using these drugs. Drug discovery and development is a broad field that encompasses many disciplines like formation of a new moiety, methodology, potency, technology and green chemistry since four decades. Modification of Fluoroquinolone series (ciprofloxacin, norfloxacin, levofloxacin, sparfloxacin and pefloxacin) is the focus of present research. Firstly, fluoroquinolone derivatives had been designed with the help of computer-assisted drug designing (CADD). Secondly, 5-substituted morpholine derivatives are synthesized. Experimental analysis, FTIR and ¹H NMR spectral data evaluated that the results are in accordance with the estimated SAR and QSAR studies i.e. newly synthesized drugs are found to be more potent with increased solubility and less side effects as compared to the parent counter fluoroquinolone drugs.