Noncytotoxic Pyrrolobenzodiazepine-Ciprofloxacin Conjugate with Activity against <i>Mycobacterium tuberculosis</i>.

ABSTRACT: The development of new antitubercular agents for the treatment of infections caused by multidrug-resistant (MDR) Mycobacterium tuberculosis is an urgent priority. Pyrrolobenzodiazepines (PBDs) are a promising class of antibacterial agents that were initially discovered and isolated from a range of Streptomyces species. Recently, C8-linked PBD monomers have been shown to work by inhibiting DNA gyrase and have demonstrated activity against M. tuberculosis. However, both PBD monomers and dimers are toxic to eukaryotic cells, limiting their development as antibacterial agents. To eliminate the toxicity associated with PBDs and explore the effect of C8-modification with a known antibacterial agent with the same mechanism of action (i.e., ciprofloxacin, a gyrase inhibitor),

SUBMITTER: Picconi P 

PROVIDER: S-EPMC6921268 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature