Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis Academic Article uri icon

Overview

MeSH Major

  • Antitubercular Agents
  • Cephalosporins
  • Mycobacterium tuberculosis
  • Tuberculosis

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.

publication date

  • July 14, 2016

Research

keywords

  • Academic Article

Identity

Language

  • eng

PubMed Central ID

  • PMC4947980

Digital Object Identifier (DOI)

  • 10.1021/acs.jmedchem.5b01833

PubMed ID

  • 27144688

Additional Document Info

start page

  • 6027

end page

  • 44

volume

  • 59

number

  • 13