Discovery and Validation of a Series of Aryl Sulfonamides as Selective Inhibitors of Tissue-Nonspecific Alkaline Phosphatase (TNAP)

We report the characterization and optimization of drug-like small molecule inhibitors of tissue-nonspecific alkaline phosphatase (TNAP), an enzyme critical for the regulation of extracellular matrix calcification during bone formation and growth. High-throughput screening (HTS) of a small molecule...

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Veröffentlicht in:	Journal of medicinal chemistry 2009-11, Vol.52 (21), p.6919-6925
Hauptverfasser:	Dahl, Russell, Sergienko, Eduard A, Su, Ying, Mostofi, Yalda S, Yang, Li, Simao, Ana Maria, Narisawa, Sonoko, Brown, Brock, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Smith, Layton H, O’Neill, W. Charles, Millán, José Luis, Cosford, Nicholas D. P
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkaline Phosphatase - antagonists & inhibitors Animals Biological and medical sciences Biological Availability Calcinosis - prevention & control Catalysis Cercopithecus aethiops COS Cells In Vitro Techniques Medical sciences Microsomes, Liver - metabolism Miscellaneous Permeability Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - pharmacokinetics Quinolines - pharmacology Rats Solubility Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - pharmacokinetics Sulfonamides - pharmacology
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