Synthesis and Antibacterial Activity of Resveratrol Derivatives

摘要

Resveratrol (3,5,4'-trihydroxy-trans-stilbene), which is a naturally occurring phytoalexin produced by a wide range of plants in response to environmental stress or pathogenic attack, is found in various medical plants. It has attracted increasing attention over the past decade because of its multiple beneficial bioac-tivity. In this paper, a set of 12 methoxylated trans-stilbene resveratrol analogues were prepared from methoxybenzoic acids. In addition, all compounds have been evaluated for their antibacterial activity against both types of Gram negative and Gram positive bacteria compared to resveratrol. Pharmacological data indicated that several derivatives showed a marked antibacterial activity, especially the most promising compound 2c, which has the low MIC 60 ～ 90 μg/mL value compared to the resveratrol. Both minimal inhibitory concentration (MIC) and inhibition zones were determined in order to monitor the efficacy of the synthesized compounds. Certain compounds inhibit bacterial growth with low MIC (μg/mL) value. The substitution pattern of the resveratrol derivatives at electronegative groups such as Cl was most important for the activity. Overall, identification of the potential efficacy of these compounds could serve as the bases for the development of novel antibacterial agents.