Novel pyridopyrazine and pyrimidothiazine derivatives as FtsZ inhibitors

Bioorg Med Chem. 2011 Dec 1;19(23):7120-8. doi: 10.1016/j.bmc.2011.09.062. Epub 2011 Oct 5.

Abstract

A series of pyridopyrazine and pyrimidothiazine derivatives have been synthesized and their activity against FtsZ from Mycobacterium tuberculosis (Mtb) and in vitro antibacterial activity against Mtb H(37)Ra and Mtb H(37)Rv are reported. Certain analogs described herein showed moderate to good inhibitory activity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Bacterial Proteins / antagonists & inhibitors*
  • Cytoskeletal Proteins / antagonists & inhibitors*
  • Disease Models, Animal
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mycobacterium tuberculosis / chemistry
  • Mycobacterium tuberculosis / drug effects
  • Mycobacterium tuberculosis / metabolism
  • Pyrazines / chemical synthesis
  • Pyrazines / chemistry
  • Pyrazines / pharmacology*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship
  • Thiazines / chemical synthesis
  • Thiazines / chemistry
  • Thiazines / pharmacology*

Substances

  • Antitubercular Agents
  • Bacterial Proteins
  • Cytoskeletal Proteins
  • FtsZ protein, Bacteria
  • Pyrazines
  • Pyridines
  • Pyrimidines
  • Thiazines