A group of novel isoindoline hybrids incorporating oxime, hydrazone, pyrazole, chalcone or aminosulfonyl pharmacophores (9–14) was designed and characterized by spectral data and elemental analyses results. All newly synthesized compounds were evaluated as COX-2 inhibitors, anti-inflammatory and analgesic agents. Six hybrid derivatives (10b, 10c, 11a, 11d, 13, 14) were moderate COX-2 inhibitors (IC₅₀ = 0.11–0.18 µM) close to standard celecoxib (IC₅₀ = 0.09 µM). The most active compounds showed outstanding in vivo anti-inflammatory activity (% edema inhibition = 41.7–50, 1 h; 40.7–67.4, 3 h; 20–46.7, 6 h) better than reference drug diclofenac (% edema inhibition = 29.2, 1 h; 22.2, 3 h; 20, 6 h). Most compounds showed significant peripheral and/or central analgesic activity. The moderate selective COX-2 inhibitor; dimethoxychalcone 11d (SI = 103) displayed excellent anti-inflammatory activity (% edema inhibition = 45.8–59.3) and increased thermal pain threshold (50–92.85%) comparable to piroxicam (75%). Molecular docking studies have been established.

A组包含肟，腙，吡唑，查耳酮或氨基磺酰基药效新颖异吲哚啉杂化物（9 - 14）的设计和特征是光谱数据和元素分析的结果。所有新合成的化合物均被评估为COX-2抑制剂，消炎药和止痛药。六个杂合衍生物（10b，10c，11a，11d，13、14）是中等COX-2抑制剂（IC ₅₀  = 0.11-0.18 µM），接近标准塞来昔布（IC ₅₀  = 0.09 µM）。活性最高的化合物在体内表现出出色的性能抗炎活性（抑制水肿百分比= 41.7–50，1小时； 40.7–67.4，3小时； 20–46.7，6 h）优于参考药物双氯芬酸（抑制水肿的百分比= 29.2，1 h; 22.2，3 h; 20、6小时）。大多数化合物显示出明显的外周和/或中枢镇痛活性。中度选择性COX-2抑制剂；与吡罗昔康（75％）相比，二甲氧基查耳酮11d（SI = 103）具有出色的抗炎活性（抑制水肿百分比= 45.8–59.3），并且增加了热痛阈值（50–92.85％）。已经建立了分子对接研究。