Rafaela Vrabie, Mariana Pinteala, Cristina M Al-Matarneh, Ioana C Marinas, Alina Nicolescu, Sergiu Shova, Mihaela Silion, Mădălina-Diana Gaboreanu, Mariana C Chifiriuc
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Unlocking the potential of trifluoromethyl pyrrole derivatives in chronic wounds management: rapid synthesis, structural insights, and potent antimicrobial activity.
Using a one-pot, three-component approach, we synthesised 25 dihydropyrrol-2-one and two 5-oxo-2,5-dihydrofuran compounds, each featuring two trifluoromethyl groups. This method emphasises timeliness and cost-effectiveness, crucial in drug development. Structural verification was conducted using NMR, FT-IR, MALDI-MS, single-crystal, and powder XRD. The antibacterial and antifungal activities of these compounds were evaluated on yeasts (Candida sp.) and bacteria, including Gram-positive (Staphylococcus aureus, a significant opportunistic pathogen, being more susceptible than S. epidermidis) and Gram-negative strains. Compounds with o-OH and m'-NO2 groups exhibited superior activity, while those with p-OH and m-OMe groups showed slightly lower but still significant activity. For furan structures, Candida albicans displayed greater sensitivity than C. parapsilosis. Additionally, 13 compounds demonstrated haemolysis below 5%, indicating low toxicity.
期刊介绍:
Journal of Enzyme Inhibition and Medicinal Chemistry publishes open access research on enzyme inhibitors, inhibitory processes, and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents.
Journal of Enzyme Inhibition and Medicinal Chemistry aims to provide an international and interdisciplinary platform for the latest findings in enzyme inhibition research.
The journal’s focus includes current developments in:
Enzymology;
Cell biology;
Chemical biology;
Microbiology;
Physiology;
Pharmacology leading to drug design;
Molecular recognition processes;
Distribution and metabolism of biologically active compounds.