Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, PO Box 11562, Egypt.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Modern University for Technology & Information MTI, Cairo, Egypt.
Future Med Chem. 2024 Feb;16(4):311-334. doi: 10.4155/fmc-2023-0280. Epub 2024 Jan 31.
Dual COX/5-LOX inhibition is a bright strategy for developing new potent and safe anti-inflammatory agents. New imines were synthesized and evaluated for their anti-inflammatory activity. The most active compounds were further investigated for their safety profile. Their molecular docking and physicochemical parameters were assessed. A new LC-MS/MS method was developed for the quantification of compound in rat plasma. Synthesized compounds were found to have anti-inflammatory activity (77-88% edema inhibition). In addition, , and showed analgesic activity (92.50, 95.71 and 96.28% protection, respectively). showed dual COX-2/5-LOX activity. Molecular docking expected the binding pattern of compounds in COX-1, COX-2 and 5-LOX active sites. The pharmacokinetic parameters of compound were also obtained.
双重 COX/5-LOX 抑制是开发新型有效且安全的抗炎药物的一个有前途的策略。新亚胺被合成并评估其抗炎活性。最活跃的化合物进一步研究其安全性概况。评估了它们的分子对接和物理化学参数。开发了一种新的 LC-MS/MS 方法用于测定大鼠血浆中化合物的含量。合成的化合物具有抗炎活性（抑制水肿 77-88%）。此外， 、 和 表现出镇痛活性（分别保护 92.50%、95.71%和 96.28%）。 显示出双重 COX-2/5-LOX 活性。分子对接预期了化合物在 COX-1、COX-2 和 5-LOX 活性部位的结合模式。还获得了化合物 的药代动力学参数。
