Taylor, Steven J.; Abeywardane, Asitha; Liang, Shuang; Muegge, Ingo; Padyana, Anil K.; Xiong, Zhaoming; Hill-Drzewi, Melissa; Farmer, Bennett; Li, Xiang; Collins, Brandon; Li, John Xiang; Heim-Riether, Alexander; Proudfoot, John; Zhang, Qiang; Goldberg, Daniel; Zuvela-Jelaska, Ljiljana; Zaher, Hani; Li, Jun; Farrow, Neil A. published the artcile< Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13>, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole, the main research area is indole derivative structure MMP 13 inhibitor arthritis.
Matrix metalloproteases (MMPs) play an important role in cartilage homeostasis under both normal and inflamed disease states and, thus, have become attractive targets for the treatment of arthritic diseases. Herein, we describe the identification of a potent, selective MMP-13 inhibitor, developed using fragment-based structure-guided lead identification and optimization techniques. Virtual screening methods identified a novel, indole-based MMP-13 inhibitor that bound into the S1′ pocket of the protein exhibiting a novel interaction pattern hitherto not observed in MMP-13 inhibitors. X-ray crystallog. structures were used to guide the elaboration of the fragment, ultimately leading to a potent inhibitor that was >100-fold selective over nine other MMP isoforms tested.
Journal of Medicinal Chemistry published new progress about Antiarthritics. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Recommanded Product: 5-Bromo-1-methyl-1H-imidazole.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem