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DOI 10.1080/14756366.2025.2513406

Медицинская библиотека · Journal of enzyme inhibition and medicinal chemistry · 2025

Unlocking the potential of trifluoromethyl pyrrole derivatives in chronic wounds management: rapid synthesis, structural insights, and potent antimicrobial activity.

Vrabie Rafaela, Pinteala Mariana, Al-Matarneh Cristina M, Marinas Ioana C, Nicolescu Alina, Shova Sergiu, Silion Mihaela, Gaboreanu Mădălina-Diana, Chifiriuc Mariana C

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Аннотация

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.

Для цитирования: Vrabie Rafaela, Pinteala Mariana, Al-Matarneh Cristina M, Marinas Ioana C, Nicolescu Alina, Shova Sergiu, Silion Mihaela, Gaboreanu Mădălina-Diana, Chifiriuc Mariana C. Unlocking the potential of trifluoromethyl pyrrole derivatives in chronic wounds management: rapid synthesis, structural insights, and potent antimicrobial activity.. Journal of enzyme inhibition and medicinal chemistry. 2025. DOI: 10.1080/14756366.2025.2513406.

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