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J Med Chem. 2016 Jul 14;59(13):6027-44. doi: 10.1021/acs.jmedchem.5b01833. Epub 2016 Jun 17.

Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.

Author information

1
Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill , Chapel Hill, North Carolina 27599, United States.
2
Public Health Research Institute, New Jersey Medical School, Rutgers, the State University of New Jersey , Newark, New Jersey 07013, United States.

Abstract

We report two series of novel cephalosporins that are bactericidal to Mycobacterium tuberculosis alone of the pathogens tested, which only kill M. tuberculosis when its replication is halted by conditions resembling those believed to pertain in the host, and whose bactericidal activity is not dependent upon or enhanced by clavulanate, a β-lactamase inhibitor. The two classes of cephalosporins bear an ester or alternatively an oxadiazole isostere at C-2 of the cephalosporin ring system, a position that is almost exclusively a carboxylic acid in clinically used agents in the class. Representatives of the series kill M. tuberculosis within macrophages without toxicity to the macrophages or other mammalian cells.

PMID:
27144688
PMCID:
PMC4947980
DOI:
10.1021/acs.jmedchem.5b01833
[Indexed for MEDLINE]
Free PMC Article

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