Design, synthesis and antibacterial activities of a series of new 2-oxaisocephems

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5293-6. doi: 10.1016/j.bmcl.2012.06.040. Epub 2012 Jun 23.

Abstract

A series of 2-oxaisocephems with a thio-substituted methyl group at the 3-position and a [2-(5-amino-1,2,4-thiadizol-3-yl)-2-(Z)-alkoxyimino]acetamido moiety at 7-position were synthesized and tested for their antibacterial activities. The analogs 17c and 17f have well-balanced potency and significantly enhanced activity as compared with the reference compound ceftazidime.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Cephalosporins / chemical synthesis
  • Cephalosporins / chemistry*
  • Cephalosporins / pharmacology
  • Drug Design*
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Cephalosporins