Biology-Oriented Drug Synthesis and Diversified Bioactivities of Fluoroquinolones and Triazine Derivatives

This proposal describes biology-oriented drug synthesis (BIODS) approach to transform commercially available pharmaceutical drugs to new chemical entities via simple organic transformations. We aim to design and synthesize libraries of compounds based on the main skeleton of a commercial drug with enhance and diversified biological activities The synthesized structural analogues will be screened for a wide range of pharmaceutical activities such as different type pharmaceutical activities would include anti-inflammatory, antibacterial and cytotoxic activities. Likewise, the synthesized compounds will also be screened for their inhibitory effect on different enzymes such as urease, -amylase, -glucosidase, xanthine oxidase and cholinesterase. These pharmacological screening of these compounds will be carried out at the International Center for Chemical and Biological Sciences (ICCBS), University of Karachi. In this study, fluoroquinolones which are broad spectrum antibiotics would be transformed to their structural analogues by incorporating medicinally important pharmacophores such as hydrazide, oxdiazole, thiazoles, oxazoles, carbazines, thiocarbazines, thioamides, sulfonamides and evaluation of their diversified bioactivities. Likewise, triazine is a core structural motif of several classes of drugs including antiangiogenic, antiviral, antiinflammatory, antiviral, antimicrobial, antimalarial, anticonvulsant, antitubercular, antihypertensive, neuroprotective agents, antidiabetic, and antineoplastic. The structural analogues of triazine containing compounds would also be synthesized and then evaluated for their biological potential. The structure elucidations of these synthetic derivatives would be carried by different spectroscopic techniques such as UV, IR, mass spectrometry 1H-, 13C-NMR and HREI-MS