Ravi K. Akula*, Shanthan R. Pamulaparthy, Pranay K. Koochana and Dharmarajan Sriram Pages 656 - 664 ( 9 )
Background: Tuberculosis is a contagious, air borne disease and second leading cause of death among infectious diseases worldwide. Fluoroquinolones are well-known antibacterial agents and they were recommended as second-line of antitubercular drugs.
Method: A series of novel fluoroquinolone analogs 6-24 was effectively synthesized. An attempt was made by tagging the substituted pyrazole on to fluoroquinolones for the first time at C-7 position. The newly synthesized compounds were characterized by FTIR, 1HNMR, ESI-MS, HR-MS and elemental analysis. The in vitro antibacterial activity of all the title compounds was investigated against various gram positive, gram negative bacterial organisms and in vitro antitubercular activity against Mycobacterium Tuberculosis H37Rv strain.
Result: Most of the synthesized compounds showed comparable activity against the entire gram positive and gram negative bacterial organisms. Fluoroquinolone 16 showed enhanced activity against both type of bacterial strains and compound 11showed promising activity against MTB-H37Rv strain.
Conclusion: Some of the novel fluoroquinolone analogs (11, 16) showed potent antibacterial, antitubercular activity.
Fluoroquinolones, Tuberculosis, Antimicrobial activity, 2-(Piperidin-4-yl)-1H-benzo[d] imidazole, pharmacokinetic, benzimidazole.
Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Biology Division (Bioinformatics), CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad- 500 007, Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500078