Urea/thiourea derivatives of quinazolinone-lysine conjugates: synthesis and structure-activity relationships of a new series of antimicrobials

Eur J Med Chem. 2011 Jun;46(6):2530-40. doi: 10.1016/j.ejmech.2011.03.041. Epub 2011 Apr 8.

Abstract

Synthesis of a series of urea/thiourea/acetamide/sulphonamide derivatives of quinazolinones conjugated lysine has been reported. Structures of the products have been determined by standard spectroscopical studies. All the compounds have been screened for their antibacterial studies and structure-activity relationship has been developed. The activity profile revealed that the compounds containing urea and thiourea functionalities along with fluoro group have exerted a highly potent activity. Thus, the title compounds represent a novel class of potent antimicrobial agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Dose-Response Relationship, Drug
  • Lysine / chemistry*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Quinazolinones / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Urea / analogs & derivatives
  • Urea / chemistry
  • Urea / pharmacology*

Substances

  • Amides
  • Anti-Bacterial Agents
  • Quinazolinones
  • Urea
  • Lysine