Synthesis and biological activity of 5-amino-and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure- …

JM Domagala, AJ Bridges, TP Culbertson…

Index: Domagala; Bridges; Culbertson; Gambino; Hagen; Karrick; Porter; Sanchez; Sesnie; Spense; Szotek; Wemple Journal of Medicinal Chemistry, 1991 ,  vol. 34,  # 3  p. 1142 - 1154

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Citation Number: 62

Abstract

A series of 5-amino-and 5-hydroxyquinolone antibacterials substituted at C7 with a select group of common piperazinyl and 3-aminopyrrolidinyl side chains was prepared. These 5- substituted derivatives were compared to the analogous 5-hydrogen compounds for antiinfective activity by using DNA gyrase inhibition, minimum inhibitory concentrations against a variety of bacteria, and in vivo efficacy in the mouse infection model. The ...