Literature DB >> 10206542

Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.

J S Plummer1, C Cai, S J Hays, J L Gilmore, M R Emmerling, W Michael, L S Narasimhan, M D Watson, K Wang, R Nath, L M Evans, J C Jaen.   

Abstract

A series of 2-sulfonyl-4H-3,1-benzoxazinones was prepared that inhibit C1r protease in vitro. Several compounds were found to be selective for C1r verses the related serine protease trypsin. Selected compounds demonstrated functional activity in a hemolysis assay.

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Year:  1999        PMID： 10206542     DOI： 10.1016/s0960-894x(99)00095-5

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


  6 in total

Review 1.  Inhibition of complement as a therapeutic approach in inflammatory central nervous system (CNS) disease.

Authors:  S R Barnum
Journal:  Mol Med       Date:  1999-09       Impact factor: 6.354

2.  Structure-based virtual screening of small-molecule antagonists of platelet integrin αIIbβ3 that do not prime the receptor to bind ligand.

Authors:  Ana Negri; Jihong Li; Sarasija Naini; Barry S Coller; Marta Filizola
Journal:  J Comput Aided Mol Des       Date:  2012-08-15       Impact factor: 3.686

3.  Iodine-mediated oxythiolation of o-vinylanilides with disulfides for the synthesis of benzoxazines.

Authors:  Yu Yang; Liyan Liu; Kuiliang Li; Zhenggen Zha; Qi Sun; Zhiyong Wang
Journal:  RSC Adv       Date:  2022-03-04       Impact factor: 3.361

4.  Lipoproteome screening of the Lyme disease agent identifies inhibitors of antibody-mediated complement killing.

Authors:  Michael J Pereira; Beau Wager; Ryan J Garrigues; Eva Gerlach; Joshua D Quinn; Alexander S Dowdell; Marcia S Osburne; Wolfram R Zückert; Peter Kraiczy; Brandon L Garcia; John M Leong
Journal:  Proc Natl Acad Sci U S A       Date:  2022-03-21       Impact factor: 12.779

5.  2-Amino- and 2-alkylthio-4H-3,1-benzothiazin-4-ones: synthesis, interconversion and enzyme inhibitory activities.

Authors:  Hans-Georg Häcker; Florian Grundmann; Friederike Lohr; Philipp A Ottersbach; Jing Zhou; Gregor Schnakenburg; Michael Gütschow
Journal:  Molecules       Date:  2009-01-14       Impact factor: 4.411

6.  Targeting the Initiator Protease of the Classical Pathway of Complement Using Fragment-Based Drug Discovery.

Authors:  Blake R Rushing; Denise L Rohlik; Sourav Roy; D Andrew Skaff; Brandon L Garcia
Journal:  Molecules       Date:  2020-09-03       Impact factor: 4.411
  6 in total

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