A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis.

摘要: Mycobacterium tuberculosis, which causes is the greatest single infectious cause of mortality worldwide, killing roughly two million people annually. Estimates indicate that one-third world population infected with latent M. tuberculosis. The synergy between tuberculosis and AIDS epidemic, surge multidrug-resistant clinical isolates have reaffirmed as a primary public health threat. However, new antitubercular drugs mechanisms action not been developed in over thirty years. Here we report series compounds containing nitroimidazopyran nucleus possess activity. After activation by mechanism dependent on F420 cofactor, nitroimidazopyrans inhibited synthesis protein cell wall lipid. In contrast to current drugs, exhibited bactericidal activity against both replicating static Lead compound PA-824 showed potent multidrugresistant promising oral animal infection models. We conclude offer practical qualities small molecule potential for treatment