REVIEW Pazufloxacin is a fused tricyclic fluoroquinoline antibacterial free base with a 1-aminocyclopropyl substituent at the C10 position. The presence of an aminoacyl group at C10 is a unique feature of the molecule, imparting potent broad spectrum activity against gram-positive and gram-negative bacteria including a variety of resistant strains and anaerobic bacteria. Pazufloxacin has shown multimodal mechanism of action and inhibits both DNA gyrase and topoisomerase IV enzyme, leading to increased antibacterial spectrum via DNA gyrase-dependent processes such as DNA polymerization, (ATP-dependent) DNA supercoiling, and chromosome fragmentation. Moreover, pazufloxacin has been shown to have DNA antagonistic actions too. The multimodal mechanism of action is linked to the low potential for the development of resistance in pazufloxacin. Moreover, it has been shown that pazufloxacin is not affected by efflux mechanism of resistance.
REFERENCES
[1]
Narita, Hirokazu; Todo, Yozo; Nitta, Jun; Takagi, Hiroyasu; Iino, Fumihiko; Miyajima, Mikako; Fukuoka, Yoshikazu; Saikawa, Isamu Preparation, testing, and formulation of oxopyridobenzoxazinecarboxylates, -benzothiazinecarboxylates, and -quinoxalinecarboxylates as antibacterials Ger. Offen. (1989), DE 3913245 A1 19891102.
Todo, Yozo; Takagi, Hiroyasu; Iino, Fumihiko; Fukuoka, Yoshikazu; Takahata, Masahiro; Okamoto, Seiki; Saikawa, Isamu; Narita, Hirokazu Pyridonecarboxylic acids as antibacterial agents. IX. Synthesis and structure-activity relationship of 3-substituted 10-(1-aminocyclopropyl)-9-fluoro-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acids and their 1-thio and 1-aza analogs. Chemical & Pharmaceutical Bulletin (1994), 42(12), 2569-74.
[4]
Todo, Yozo; Takagi, Hiroyasu; Iino, Fumihiko; Hayashi, Kazuya; Takata, Makoto; Kuroda, Hiroshi; Momonoi, Kaishu; Narita, Hirokazu Practical synthesis of T-3761, (S)-10-(1-aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid Chemical & Pharmaceutical Bulletin (1994), 42(12), 2629-32.
[5]
Muratani T, Inoue M, Mitsuhashi S. In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother. 1992 Oct;36(10):2293-303.
[6]
Fukuoka Y, Ikeda Y, Yamashiro Y, Takahata M, Todo Y, Narita H. In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimicrob Agents Chemother. 1993 Mar;37(3):384-92.
[7]
Johnson AP. Pazufloxacin Toyama Chemical Co. Curr Opin Investig Drugs. 2000 Sep;1(1):52-7.
[8]
Minami S, Hattori R, Matsuda A. Pharmacological properties and expected clinical role of an injectable new quinolone antibiotic, pazufloxacin mesilate]. Nihon Yakurigaku Zasshi. 2003 Aug;122(2):161-78.
[9]
Andersson MI, MacGowan MP. Development of the quinolones. Journal of Antimicrobial Chemotherapy 2003; 51:1-11.
[10]
Hawkey PM. Mechanisms of quinolone action and microbial response. Journal of Antimicrobial Chemotherapy 2003; 51:29-35.
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