Compounds > 2-5-dimethoxy-n-(quinolin-3-yl)benzenesulfonamide

2-5-dimethoxy-n-(quinolin-3-yl)benzenesulfonamide and Calcinosis

2-5-dimethoxy-n-(quinolin-3-yl)benzenesulfonamide has been researched along with Calcinosis* in 1 studies

Other Studies

1 other study(ies) available for 2-5-dimethoxy-n-(quinolin-3-yl)benzenesulfonamide and Calcinosis

Article	Year
Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Journal of medicinal chemistry, 2009, Nov-12, Volume: 52, Issue:21 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 library led to the identification of arylsulfonamides as potent and selective inhibitors of TNAP. Critical structural requirements for activity were determined, and the compounds were subsequently profiled for in vitro activity and bioavailability parameters including metabolic stability and permeability. The plasma levels following subcutaneous administration of a member of the lead series in rat was determined, demonstrating the potential of these TNAP inhibitors as systemically active therapeutic agents to target various diseases involving soft tissue calcification. A representative member of the series was also characterized in mechanistic and kinetic studies. Topics: Alkaline Phosphatase; Animals; Biological Availability; Calcinosis; Catalysis; Chlorocebus aethiops; COS Cells; In Vitro Techniques; Microsomes, Liver; Permeability; Quinolines; Rats; Solubility; Structure-Activity Relationship; Sulfonamides	2009

Article

Year

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).

Journal of medicinal chemistry, 2009, Nov-12, Volume: 52, Issue:21

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 library led to the identification of arylsulfonamides as potent and selective inhibitors of TNAP. Critical structural requirements for activity were determined, and the compounds were subsequently profiled for in vitro activity and bioavailability parameters including metabolic stability and permeability. The plasma levels following subcutaneous administration of a member of the lead series in rat was determined, demonstrating the potential of these TNAP inhibitors as systemically active therapeutic agents to target various diseases involving soft tissue calcification. A representative member of the series was also characterized in mechanistic and kinetic studies.

Topics: Alkaline Phosphatase; Animals; Biological Availability; Calcinosis; Catalysis; Chlorocebus aethiops; COS Cells; In Vitro Techniques; Microsomes, Liver; Permeability; Quinolines; Rats; Solubility; Structure-Activity Relationship; Sulfonamides

2009