Yiman Qin, Guanyi Li, Ling Wang, Guangyuan Yin, Xiang Zhang, Hongxiang Wang, Pengfei Zheng, Wentao Hua, Yan Cheng, Yaxue Zhao, Jiong Zhang
Hyaluronidase is a promising target in drug discovery, given its overexpression in a range of physiological and pathological processes, including tumor migration, skin aging, sagging, and wrinkling, as well as inflammation and bacterial infections. In this study, to identify novel hyaluronidase inhibitors, we applied click chemistry for the modular synthesis of 370 triazoles in 96-well plates, starting with biphenyl azide. Utilizing an optimized turbidimetric screening assay in microplates, we identified Fmoc-containing triazoles 5 and 6, as well as quinoline-containing triazoles 15 and 16, as highly effective hyaluronidase inhibitors...
March 16, 2024: Bioorganic Chemistry