| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370621 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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 moiety increased activity over the 2,3-unsubstituted derivative. Energy minimization of structures provides an explanation for relative activities of fluoroquinolones having a C-2 thio moiety.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kevin R. Marks, Muhammad Malik, Arkady Mustaev, Hiroshi Hiasa, Karl Drlica, Robert J. Kerns,