In this study, responses of rice under drought stress correlating with changes in chemical compositions were examined. Among 20 studied rice cultivars, Q8 was the most tolerant, whereas Q2 was the most susceptible to drought. Total phenols, total flavonoids, and antioxidant activities, and their accumulation in water deficit conditions were proportional to drought resistance levels of rice. In detail, total phenols and total flavonoids in Q8 (65.3 mg gallic acid equivalent (GAE) and 37.8 mg rutin equivalent (RE) were significantly higher than Q2 (33.9 mg GAE/g and 27.4 mg RE/g, respectively) in both control and drought stress groups. Similarly, the antioxidant activities including DPPH radical scavenging, β-carotene bleaching, and lipid peroxidation inhibition in Q8 were also higher than in Q2, and markedly increased in drought stress. In general, contents of individual phenolic acids in Q8 were higher than Q2, and they were significantly increased in drought stress to much greater extents than in Q2. However, p-hydroxybenzoic acid was found uniquely in Q8 cultivars. In addition, only vanillic acid was found in water deficit stress in both drought resistant and susceptible rice, suggesting that this phenolic acid, together with p-hydroxybenzoic acid, may play a key role in drought-tolerance mechanisms of rice. The use of vanillic acid and p-hyroxybenzoic acid, and their derivatives, may be useful to protect rice production against water shortage stress.