Antimicrobial prospect of newly synthesized 1,3-thiazole derivatives

Bassem Sadek, Moawia Mohammad Al-Tabakha, Khairi Mustafa Salem Fahelelbom

Research output: Contribution to journalArticlepeer-review

33 Citations (Scopus)

Abstract

A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10-15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25-200 μg/mL against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram-ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125-200 μg/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50-75 μg/mL) against the Gram+ve, Gram-ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4.

Original languageEnglish
Pages (from-to)9386-9396
Number of pages11
JournalMolecules
Volume16
Issue number11
DOIs
Publication statusPublished - Nov 2011

Keywords

  • 1,3-thiazoles
  • Antimicrobial evaluation
  • Partition coefficient
  • Synthesis
  • benzo[d]thiazoles

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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