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 ...
[Nguyen, Son T.; Ding, Xiaoyuan; Butler, Michelle M.; Tashjian, Tommy F.; Peet, Norton P.; Bowlin, Terry L. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5961 - 5963]
