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Medicinal Chemistry

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ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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Research Article

Synthesis and Biological Evaluation of 3-cyano-4H-chromene Derivatives Bearing Carbamate Functionality

Author(s): Fatma Boukattaya, Amal Daoud, Fabien Boeda, Morwenna S.M. Pearson-Long, Néji Gharsallah, Adel Kadri, Philippe Bertus* and Houcine Ammar

Volume 15, Issue 3, 2019

Page: [257 - 264] Pages: 8

DOI: 10.2174/1573406414666181009124449

Price: $65

Abstract

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.

Keywords: Antibacterial activity, Antifungal activity, Carbamates, Chromenes, Coumarins, Grignard reagents.

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