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1-Aryl-3-(1H-imidazol-1-yl)propan-1-ol esters: synthesis, anti-Candida potential and molecular modeling studies

Mohamed I Attia1, Awwad A Radwan, Azza S Zakaria

  • 1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P,O, Box 2457, Riyadh 11451, Saudi Arabia. mattia@ksu.edu.sa.

Chemistry Central Journal
|October 26, 2013
PubMed
Abstract

Insights

New esters demonstrate potent anti-Candida activity, outperforming fluconazole. Compound 5a showed significant efficacy against Candida infections, offering a promising alternative for treating fungal diseases.

Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Drug Discovery

Background:

  • Rising incidence of invasive and superficial fungal infections globally.
  • Candida species are a major cause of hospital-acquired fungal infections.
  • Candida albicans causes most invasive Candida infections, with high mortality rates.

Purpose of the Study:

  • Synthesize novel aromatic and heterocyclic esters.
  • Evaluate the anti-Candida potential of synthesized compounds.
  • Investigate compounds for activity against Candida albicans.

Main Methods:

  • Synthesis of 1-aryl-3-(1H-imidazol-1-yl)propan-1-ol esters (5a-k).
  • Antifungal activity evaluation using Minimum Inhibitory Concentration (MIC) assays.
  • Molecular modeling studies to assess pharmacophore geometry.

Main Results:

  • Compound 5a exhibited potent anti-Candida activity with an MIC of 0.0833 μmol/mL.
  • The synthesized esters (5a-k) showed superior activity compared to fluconazole.
  • Compounds 7 and 8 demonstrated significant anti-Candida albicans activity.

Conclusions:

  • Newly synthesized esters possess potent anti-Candida activity.
  • Compounds 7 and 8 effectively match proposed pharmacophore models.
  • These novel esters represent promising candidates for antifungal drug development.

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