Literature DB >> 19329309

Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.

Darrin W Hopper1, Matthew D Vera, David How, Joshua Sabatini, Jason S Xiang, Manus Ipek, Jennifer Thomason, Yonghan Hu, Eric Feyfant, Qin Wang, Katy E Georgiadis, Erica Reifenberg, Richard T Sheldon, Cristin C Keohan, Manas K Majumdar, Elisabeth A Morris, Jerauld Skotnicki, Phaik-Eng Sum.   

Abstract

The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation of a series of biphenylsulfonamides resulted in the identification of the ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides analogs (19-21 and 24) with improved Agg-1 inhibition and MMP-2, MMP-13 activity.

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Year:  2009        PMID: 19329309     DOI: 10.1016/j.bmcl.2009.03.056

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).

Authors:  Yun Ding; Heather O'Keefe; Jennifer L DeLorey; David I Israel; Jeffrey A Messer; Cynthia H Chiu; Steven R Skinner; Rosalie E Matico; Monique F Murray-Thompson; Fan Li; Matthew A Clark; John W Cuozzo; Christopher Arico-Muendel; Barry A Morgan
Journal:  ACS Med Chem Lett       Date:  2015-07-07       Impact factor: 4.345

2.  Pharmacophore development and screening for discovery of potential inhibitors of ADAMTS-4 for osteoarthritis therapy.

Authors:  Priyanka Verma; Krishna Dalal; Madhu Chopra
Journal:  J Mol Model       Date:  2016-07-11       Impact factor: 1.810

3.  Structure analysis reveals the flexibility of the ADAMTS-5 active site.

Authors:  Huey-Sheng Shieh; Alfredo G Tomasselli; Karl J Mathis; Mark E Schnute; Scott S Woodard; Nicole Caspers; Jennifer M Williams; James R Kiefer; Grace Munie; Arthur Wittwer; Anne-Marie Malfait; Micky D Tortorella
Journal:  Protein Sci       Date:  2011-04       Impact factor: 6.725

4.  Room temperature synthesis and antibacterial activity of new sulfonamides containing n,n-diethyl-substituted amido moieties.

Authors:  Olayinka O Ajani; Oluwole B Familoni; Feipeng Wu; Johnbull O Echeme; Zheng Sujiang
Journal:  Int J Med Chem       Date:  2012-10-17
  4 in total

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