Preparation, Gram-Negative Antibacterial Activity, and Hydrolytic Stability of Novel Siderophore-Conjugated Monocarbam Diols
Mark E. Flanagan, Steven J. Brickner, Manjinder S. Lall, Jeffrey Casavant, Laura A. Deschenes, Steven M. Finegan, D. M. George, Karl Granskog, Joel R. Hardink, Michael D. Huband, Trong-Trieu Hoang, Lucinda Lamb, Andrea Marra(Melinta Therapeutics (United States)), Mark J. Mitton‐Fry, John P. Mueller, Lisa Mullins, Mark C. Noe, John P. O’Donnell, David Pattavina, Joseph Penzien, Brandon P. Schuff, Jianmin Sun, David A. Whipple(University of Kansas), Jennifer A. Young, Thomas D. Gootz
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Abstract
A novel series of monocarbam compounds exhibiting promising antibacterial activity against multidrug resistant Gram-negative microorganisms is reported, along with the synthesis of one such molecule MC-1 (1). Also reported are structure-activity relationships associated with the in vitro and in vivo efficacy of 1 and related analogues in addition to the hydrolytic stability of such compounds and possible implications thereof.
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