Synthesis and QSAR studies on 5-[2-(2-methylprop1-enyl)-1H benzimidazol-1yl]-4,6-diphenyl-pyrimidin-2-(5H)-thione derivatives as antibacterial agents

Eur J Med Chem. 2006 Jul;41(7):833-40. doi: 10.1016/j.ejmech.2006.03.022. Epub 2006 May 26.

Abstract

A new series of 5-[2-(2-methylprop1-enyl)-1H benzimidazol-1yl]-4,6-diphenyl-pyrimidin-2-(5H)-thione derivatives [3a-q] has been synthesized and subjected to evaluate their antibacterial properties. All the synthesized compounds of the series displayed, remarkable activity in comparison to standard drug (ampicillin). A number of descriptors were tested to adjudge a quantitative correlation between activity and structural features. However, significant correlations have emerged between activity and physicochemical parameters viz. polarizability parameter (MR). Moreover, results are interpreted on the basis of multiple regression and cross-validation methodology.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacillus subtilis / drug effects
  • Gram-Negative Bacteria / drug effects
  • Models, Molecular
  • Molecular Structure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Quantitative Structure-Activity Relationship
  • Staphylococcus aureus / drug effects
  • Thiones / chemical synthesis*
  • Thiones / chemistry
  • Thiones / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Pyrimidines
  • Thiones