DESIGN, SYNTHESIS AND COMPARATIVE PHARMACOLOGICAL ASSESSMENT OF NOVEL FLUOROQUINOLONE DERIVATIVESAbstract
One of the proposed groupings of the fluoroquinolones describes the excellent broad-spectrum activity forms an invaluable part of the present anti-infective armory of the clinicians. The fluoroquinolones are most significant weapons can be credited for saving more human lives than any other area of medicinal therapy. In this current research segment, the novel C-3 substituted fluoroquinolone scaffolds were designed, synthesized and elucidated by IR, H1NMR, and MS spectral data. The clinically banned drug gatifloxacin is acting as starting material used to obtain targeted compounds. The proposed scheme comprised of main cyclization by using phosphorous oxychloride, thiosemicarbazide, gatifloxacin. The former compounds were undergoing diazotization reaction followed by a coupling reaction with various tertiary amines. Further, all seven 3- substituted gatifloxacin derivatives (PGI-PGVII) were screened for antimicrobial and hypoglycemic activity. In the novel series of compounds PG III, PG IV, PG V exhibited good antimicrobial activity by inhibition of DNA gyrase enzyme whereas PG I, PG III, PG VI, PG VII were found to be the most active compounds with hypoglycemic activity.
P. P. Majalekar *, P. K. Shirote, V. Nalawade and P. Shelake
Department of Pharmaceutical Chemistry, Appasaheb Birnale College of Pharmacy, Sangli, Maharashtra, India.
08 December 2018
06 July 2019
13 July 2019
01 August 2019