Pleuromutilins. Part 1. The identification of novel mutilin 14-carbamates

Bioorg Med Chem. 2001 May;9(5):1221-31. doi: 10.1016/s0968-0896(00)00338-2.

Abstract

A novel series of mutilin 14-carbamates has been discovered as a result of structure-activity studies on the naturally occurring antibiotic pleuromutilin (1). In particular, the 4-methoxybenzoylcarbamate, SB-222734 (15o) displays potent antibacterial activity against a number of bacterial pathogens which are resistant to currently used agents and shows enhanced metabolic stability when compared to earlier pleuromutilin derivatives. Such derivatives therefore have the potential to provide a new class of antibacterial agents for human therapy which address the threat of bacterial resistance.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology*
  • Biological Factors / chemistry
  • Biological Factors / pharmacology
  • Carbamates / chemical synthesis
  • Carbamates / pharmacology
  • Diterpenes / chemical synthesis*
  • Diterpenes / pharmacology*
  • Drug Resistance, Microbial / genetics
  • Drug Resistance, Microbial / physiology
  • Haemophilus influenzae / drug effects*
  • Microbial Sensitivity Tests / standards
  • Polycyclic Compounds
  • Staphylococcus / drug effects*

Substances

  • Anti-Bacterial Agents
  • Biological Factors
  • Carbamates
  • Diterpenes
  • Polycyclic Compounds
  • mutilin 14-(N-(4-methoxybenzoyl))-carbamate
  • pleuromutilin
  • tiamulin