Discovery of Safe COX-2 Inhibitors: Achieving Reduced Colitis Side Effects through Balanced COX Inhibition.

• Tác giả: Zhiran Ju, Qin Li, Junhui Wu, Xinlin Zhu
• Ngôn ngữ: eng
• Ký hiệu phân loại: 615.43 Pills, capsules, tablets, troches, powders
• Thông tin xuất bản: Germany : ChemMedChem , 2025
• Bộ sưu tập: NCBI
• ID: 753576

Tóm tắt

The severe adverse effects associated with imbalanced cyclooxygenase-2 (COX-2) inhibition continue to pose significant challenges in the development of contemporary anti-inflammatory drugs. In recent years, the approach to COX-2 inhibitor drug development has shifted from a focus on highly selective inhibition of COX-2 to a strategy that emphasizes more moderate selectivity. The amino acid sequence and structural similarities between inducible COX-2 and constitutive cyclooxygenase-1 (COX-1) isoforms present both substantial opportunities and challenges for the design of next generation of balanced COX-2 inhibitors. As part of our ongoing research into the discovering novel and safer COX-2 inhibitors, we reported herein a highly potent and balanced COX-2 inhibitor 21 d (IC