Patents on DNA gyrase inhibitors: January 1995 to March 1998

This review summarises patents claiming novel DNA gyrase inhibitors (quinolones and non-quinolones) published from January 1995 to date. The majority of these patents describe the synthesis and biological evaluation of new fluoroquinolone analogues with modified substituents on N-1, C-5, C-7 or C-8 of the quinolone ring system. A series of quinolizinones were reported as potent broad-spectrum antibacterial agents with activity against several resistant bacterial strains. Two interesting non-quinolone inhibitors with new chemotypes were reported. However, no detailed reports on biological profiles were described. Several patents relating to the improved synthesis of quinolone intermediates were also published. The last group of patents reported new formulation methods for known quinolones, which claimed to provide improved physical stability or improved therapeutic efficacy. New applications of known fluoroquinolones against aphthous ulcers and human immunodeficiency virus (HIV) were also claimed.