rifalazil

Rifalazil is a small molecule antibiotic of the ansamycin class and a derivative of rifamycin. It acts by inhibiting bacterial DNA-dependent RNA polymerase, specifically blocking the β-subunit, which results in potent bactericidal activity against *Mycobacterium tuberculosis* and other gram-positive bacteria. Rifalazil was developed as a potential replacement for rifampin in tuberculosis therapy due to its superior antimicrobial activity and long half-life, allowing for less frequent dosing. It also showed promise in treating infections caused by *Chlamydia trachomatis* (including non-gonococcal urethritis and cervicitis), *Chlamydia pneumoniae* (potentially linked to chronic inflammatory diseases such as atherosclerosis), *Helicobacter pylori* (gastric ulcer disease), and *Clostridioides difficile* (antibiotic-associated colitis). Despite reaching phase III clinical trials, development was terminated in 2013 due to severe side effects[1][2][3][5].

Other names

benzoxazinorifamycin3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin