An overview on antitubercular activity profile of fluoroquinolone derivatives and their molecular hybridization

Tuberculosis (TB) has been one of the main causes of morbidity, and the emergence of multi-drug resistant (MDR) Mycobacterium tuberculosis strains has become a major concern. The decrease in activity of the major anti-TB drugsincluding, isoniazid, and rifampicin is an important threat that requires an urgent therapy. Anti-TB activity of the fluoroquinolones (FQs) has been under investigation. Many FQs are active in vitro; however, only a few such as ofloxacin, ciprofloxacin, sparfloxacin, levofloxacin, Moxifloxacin, and gatifloxacin have been clinically tested. The FQs can be used in co-therapy with the available anti-TB drugs. Molecular hybridization is a concept of drug design and development based on combination of pharmacophoric moieties of various bioactive compounds to produce a new hybrid compound with improved affinity and efficacy compared with the present drugs.

Keywords:

Fluoroquinolones , Tuberculosis , Ofloxacin , Ciprofloxacin , sparfloxacin , Levofloxacin