| DOI: https://doi.org/10.14456/mujps.2016.5 | Pharm Sci Asia 2016; 43(1), 45-53 |
Synthesis and antimicrobial activity screening of 2-(2-fluorophenylimino)-5-arylidenethiazolidin-4-one derivativesD.T. Pham*, T.M.H. Vo, P. Truong, P.T. Ho, N. Khorana
1 Department of Pharmaceutical Technology, Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, Vietnam
2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, Can Tho, Vietnam
3 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh city, Vietnam
4 Department of Pharmaceutical Technology and Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok,Thailand.
Twelve derivatives of 2-(2-fluorophenylimino)-5-arylidenethiazolidin-4-one (F1-F12) were synthesized using 2-fluoroaniline as a reactant through 3-step process including acylation reaction, cyclisation reaction and aldol condensation reaction. All synthesized compounds were elucidated the structure by infrared (IR), ultraviolet (UV), nuclear magnetic resonance (NMR) and mass spectra (MS). None of the synthesized compounds inhibited Candida albicans or Aspergillus niger. Compounds F4 and F8 showed antibacterial activity on Staphylococcus aureus with MIC ≤ 64 μg/ml and methicillin-resistant Staphylococcus aureus (MRSA) with MIC ≤ 64 μg/ml. These compounds have potential for further investigation and modification to become potential therapeutic drugs in the future.
Keyword:
thiazolidin-4-one, synthesis, antibacterial, antifungal, MRSA
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