Title:Synthesis and In vitro Antibacterial, Antitubercular Studies of Novel Fluoroquinolones Analogs Containing 4-substituted Sec Amine
VOLUME: 14
Author(s):Ravi Kumar Akula*, Shanthan Rao Pamulaparthy, Pranay Kumar Koochana, Yogeeswari Perumal and Sriarm Dharmarajan
Affiliation:CSIR-Indian Institute of Chemical Technology, Chief-Scientist, Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, CSIR-IICT - Biology Hyderabad, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad - Medicinal Chemistry Hyderabad, Telangana, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad - Medicinal Chemistry Hyderabad, Telangana
Keywords:Fluoroquinolones; Tuberculosis; Antimicrobial activity;
2-(piperidin-4-yl)-1H-benzo[d] imidazole
Abstract: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.
