Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones

KR Marks, M Malik, A Mustaev, H Hiasa, K Drlica…

Index: Marks, Kevin R.; Malik, Muhammad; Mustaev, Arkady; Hiasa, Hiroshi; Drlica, Karl; Kerns, Robert J. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 15 p. 4585 - 4588

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Citation Number: 3

Abstract

Novel fluoroquinolone derivatives substituted with a 2-thioalkyl moiety, with and without a concomitant 3-carboxylate group, were synthesized to evaluate the effect of C-2 thioalkyl substituents on gyrase binding and inhibition. The presence of a 2-thioalkyl group universally decreased activity as compared to parent fluoroquinolones. However, with derivatives of moxifloxacin the presence of either a 2-thioalkyl group or a 3-carboxylate ...