《Design and Synthesis of Water-Soluble and Potent MMP-13 Inhibitors with Activity in Human Osteosarcoma Cells》 was written by Zapico, Jose Maria; Acosta, Lourdes; Pastor, Miryam; Rangasamy, Loganathan; Marquez-Cantudo, Laura; Coderch, Claire; Ortin, Irene; Nicolau-Sanus, Maria; Puchades-Carrasco, Leonor; Pineda-Lucena, Antonio; Majali-Martinez, Alejandro; Ramos, Pilar; de Pascual-Teresa, Beatriz; Ramos, Ana. Category: triazolesThis research focused onwater soluble MMP13 inhibitor activity human osteosarcoma cell; MMP-13 inhibitors; RMN; metalloproteinases; molecular modeling; organic synthesis; osteoarthritis. The article conveys some information:
Osteoarthritis is a degenerative disease, often resulting in chronic joint pain and commonly affecting elderly people. Current treatments with anti-inflammatory drugs are palliative, making the discovery of new treatments necessary. The inhibition of matrix metalloproteinase MMP-13 is a validated strategy to prevent the progression of this common joint disorder. We recently described polybrominated benzotriazole derivatives with nanomolar inhibitory activity and a promising selectivity profile against this collagenase. In this work, we have extended the study in order to explore the influence of bromine atoms and the nature of the S1′ heterocyclic interacting moiety on the solubility/selectivity balance of this type of compound Drug target interactions have been assessed through a combination of mol. modeling studies and NMR experiments Compound 9a has been identified as a water-soluble and highly potent inhibitor with activity in MG-63 human osteosarcoma cells.Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8Category: triazoles) was used in this study.
Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8) is a polytriazolylamine ligand which stabilizes Cu(I) towards disproportionation and oxidation thus enhancing its catalytic effect in the azide-acetylene cycloaddition.Category: triazoles
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics