article · Green Chemistry Letters and Reviews
This research outlines a green organic synthesis method to produce hydrazono-thiazolone derivatives using thiamine hydrochloride, also known as Vitamin B1, as an eco-friendly catalyst. Hydrazono-thiazolones are recognised as versatile therapeutic core units with potential applications against viral, fungal, tubercular, and cancerous targets. The investigation synthesised a series of compounds, labelled 6a through 6l, and evaluated their biological performance in vitro against both Gram-positive and Gram-negative bacterial species. Minimum inhibitory concentration assessments identified compounds 6d, 6e, 6j, and 6k as possessing broad-spectrum antibacterial activity, with candidates 6j and 6k demonstrating efficacy close to that of the antibiotic ciprofloxacin. Computational molecular docking supported these results by revealing strong binding modes to Escherichia coli DNA gyrase, while pharmacokinetic simulations showed favourable drug absorption, distribution, metabolism, and excretion profiles.
Bacterial resistance to existing medicines creates an ongoing demand for new antibiotics. At the same time, chemical manufacturing often relies on toxic or unsustainable catalysts. By employing a common vitamin as a green catalyst to generate drug candidates that perform comparably to standard antibiotics, this work demonstrates a more sustainable pathway for producing potent, medically useful compounds.
This work represents early-stage laboratory discovery that could interest pharmaceutical developers and medicinal chemists seeking sustainable synthetic routes for drug discovery. The findings identify candidate molecules targeting bacterial infections, but commercial development would require progression from in vitro and in silico testing to extensive in vivo evaluation and formal preclinical safety studies.
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The study focuses on green methodologies in synthetic organic chemistry, emphasizing the use of thiamine hydrochloride (Vitamin B1) as an eco-friendly catalyst for synthesizing hydrazono-thiazolones. These compounds serve as versatile core units with various therapeutic activities, including anti-HIV, anti-tubercular, antifungal, antiviral, and anticancer properties. Building on prior research involving sustainable barium oxide-chitosan nanocomposite catalysts, this novel green synthetic approach contributes to the sustainable synthesis of bioactive heterocycles. The synthesized compounds 6a-l were tested in vitro against different bacterial species, revealing notable activity against Gram-positive and Gram-negative bacteria. The MIC investigation showed that compounds 6d, 6e, 6j, and 6k have broad-spectrum antibacterial potential, with 6j and 6k being especially effective, their MICs near those of ciprofloxacin, highlighting their strong antibacterial capabilities. Molecular docking studies predicting the binding mode of the most potent substances to Escherichia coli DNA gyrase (PDB ID 4DUH) aligned well with in vitro studies, confirming the new ligands’ potency as potential antimicrobial agents. In silico investigations for the most potent substances revealed a favorable ADME profile, suggesting promising pharmacological properties. This research contributes to both sustainable synthesis and potential therapeutic applications of hydrazono- thiazolone derivatives.
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DOI: 10.1080/17518253.2024.2380746
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