Boukattaya Fatma, Daoud Amal, Boeda Fabien, Pearson-Long Morwenna S M, Gharsallah Néji, Kadri Adel, Bertus Philippe, Ammar Houcine
Laboratoire de Chimie Appliquee: Heterocycles, Corps Gras et Polymères, Faculty of Science of Sfax, University of Sfax, BP1171, Sfax, Tunisia.
Le Mans Universite (Universite du Maine), CNRS UMR 6283, Institut des Molecules et Materiaux du Mans (IMMM), 72085 Le Mans Cedex 09, France.
Med Chem. 2019;15(3):257-264. doi: 10.2174/1573406414666181009124449.
2-Aminochromene derivatives display important pharmacological properties, including mainly antibiotic and anticancer activities.
The study aims to synthesize new chromene derivatives via a new approach using Grignard reagents, for the evaluation of their antibiotic and antifungal properties.
A series of novel 3-cyano-4-aminochromene derivatives bearing alkyl substituents at the 4-position was prepared for biological evaluation.
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.
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.
2-氨基色烯衍生物具有重要的药理特性，主要包括抗菌和抗癌活性。
本研究旨在通过一种使用格氏试剂的新方法合成新的色烯衍生物，以评估其抗菌和抗真菌特性。
制备了一系列在4-位带有烷基取代基的新型3-氰基-4-氨基色烯衍生物用于生物学评价。
通过将各种格氏试剂加入N-乙氧羰基-3-氰基亚氨基香豆素中，以中等至良好的产率（72-96%）得到了这些化合物。该反应具有完全的区域选择性。使用琼脂稀释法对新的色烯衍生物针对一组六种细菌和三种真菌菌株的体外抗菌活性进行了筛选。
色烯衍生物对革兰氏阳性菌的抗菌活性比对革兰氏阴性菌更明显，对金黄色葡萄球菌观察到显著活性。还注意到对镰刀菌属和尖孢镰刀菌有有趣的抗真菌活性。
