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Resveratrol (3, 4′, 5 trihydroxy stilbene) is a natural phytoalexin produced by plants in response to biotic and abiotic stresses. It is well known for its cardio-protective, anticarcinogenic, and antioxidant properties. This study characterized physiological and molecular changes in resveratrol synthesis exposed to two levels of water stress at distinct grape berry developmental stages. Physiological data were measured to assess the berry quality. We used high-performance liquid chromatography to study enzyme activity and qRT-PCR to assess the expression levels of genes involved in resveratrol synthesis. The berry development was suppressed under water stress, while the content of total polyphenol, especially resveratrol was enhanced. Related enzymes and genes regulate the changes in resveratrol in plants. Water stress improved the enzyme activities of PAL (phenylalanine ammonia-lyase) and STS (stilbene synthase) after veraison. Moreover, the transcription factors <i>VvMYB14, VvMYB15</i> and resveratrol synthesis-related genes are also changed. Expression of <i>Vv4CL</i> and <i>VvMYB15</i> were upregulated during the pre-reversion stage, whereas <i>VvPAL</i> and <i>VvSTS</i> increased throughout development. As the co-substrate of <i>VvSTS, VvCHS</i> decreased during the berry development. Our study demonstrates that water stress regulates resveratrol synthesis through enzymatic activities and the gene expression of PAL and STS.