Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1, 8-naphthyridine-3-carboxylic acids

JP Sanchez, JM Domagala, SE Hagen…

Index: Sanchez, Joseph P.; Domagala, John M.; Hagen, Susan E.; Heifetz, Carl L.; Hutt, Marland P.; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, p. 983 - 991

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Citation Number: 124

Abstract

Figure 1. Clinicially significant quinolone type antibacterial agents. a substituted 3- (aminomethy1) pyrrolidine substituent, at C-7.'" This slight structural modification greatly increased the Gram-positive potency, finally establishing the quinolones as a truly broad- spectrum class of antibacterial agents. In an attempt to enhance oral activity, a fluorine was introduced at C-8, which resulted in CI-934 (15), the most potent Gram-positive quinolone ...

~85%

~85%

~73%

~90%

1-Substituted 7-[3-[(ethylamino) methyl]-1-pyrrolidinyl]-6, ...

[Domagala, John M.; Heifetz, Carl L.; Hutt, Marland P.; Mich, Thomas F.; Nichols, Jeffry B.; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 5 p. 991 - 1001]