Effect of lipophilicity at N-1 on activity of fluoroquinolones against mycobacteria

…, JA Dever, SJ Gracheck, JM Domagala

Index: Renau, Thomas E.; Sanchez, Joseph P.; Shapiro, Martin A.; Dever, Julie A.; Gracheck, Stephen J.; Domagala, John M. Journal of Medicinal Chemistry, 1995 ,  vol. 38,  # 15  p. 2974 - 2977

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Citation Number: 50

Abstract

The dramatic increase in drug resistant Mycobacterium tuberculosis has caused a resurgence in research targeted toward these organisms. As part of a systematic study to optimize the quinolone antibacterials against mycobacteria, we have prepared a series of Nl- phenylsubstituted derivatives to explore the effect of increasing lipophilicity on potency at this position. The compounds, synthesized by the modification of a literature procedure, ...