Chu D T, Fernandes P B, Claiborne A K, Gracey E H, Pernet A G
J Med Chem. 1986 Nov;29(11):2363-9. doi: 10.1021/jm00161a036.
Novel arylfluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids have been prepared and their antibacterial activity evaluated. These derivatives are characterized by having a fluorine atom at the 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position. The in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or o,p-difluorophenyl and the 7-substituent is a 3-amino-1-pyrrolidinyl group. 1-(2,4-Difluorophenyl)-6-fluoro-7-(3-amino-1-pyrrolidinyl)-1,4-dihydro- 4-oxo-1,8-naphthyridine-3-carboxylic acid (38) was found to possess excellent in vitro potency and in vivo efficacy.
新型芳基氟代-1,4-二氢-4-氧代-1,8-萘啶-3-羧酸已被制备并评估了其抗菌活性。这些衍生物的特征在于在6位有一个氟原子，在7位有取代氨基，在1位有取代苯基。当1-取代基为对氟苯基或邻、对二氟苯基且7-取代基为3-氨基-1-吡咯烷基时，体外抗菌效力最大。发现1-(2,4-二氟苯基)-6-氟-7-(3-氨基-1-吡咯烷基)-1,4-二氢-4-氧代-1,8-萘啶-3-羧酸(38)具有优异的体外效力和体内疗效。
