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Article Dans Une Revue Medicinal Chemistry Année : 2018

Synthesis and biological evaluation of 3-cyano-4H-chromene derivatives bearing carbamate functionality

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Résumé

Background: 2-Aminochromene derivatives display important pharmacological properties, including mainly antibiotic and anticancer activities. Objective: The study aims to synthesize new chromene derivatives via a new approach using Grignard reagents, for the evaluation of their antibiotic and antifungal properties. Method: A series of novel 3-cyano-4-aminochromene derivatives bearing alkyl substituents at the 4-position was prepared for biological evaluation. Results: These compounds were obtained by the addition of various Grignard reagents into Nethoxycarbonyl- 3-cyanoiminocoumarines in moderate to good yields (72-96%). The reaction is completely regioselective. The new chromene derivatives were screened for their in vitro antimicrobial activities against a panel of six bacterial and three fungal strains using agar dilution method. Conclusion: The antibacterial activity of the chromene derivatives was more pronounced on Gram-positive bacteria than on Gram-negative bacteria with a significant activity observed against Staphylococcus aureus. An interesting antifungal activity against Fusarium sp. and Fusarium oxysporum was also noticed.
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Dates et versions

hal-01921815 , version 1 (14-11-2018)

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Fatma Boukattaya, Amal Daoud, Fabien Boeda, Morwenna Pearson-Long, Neji Gharsallah, et al.. Synthesis and biological evaluation of 3-cyano-4H-chromene derivatives bearing carbamate functionality. Medicinal Chemistry, 2018, 14, ⟨10.2174/1573406414666181009124449⟩. ⟨hal-01921815⟩
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