Literature DB >> 30034585

Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.

Laurent Knerr1, Fabrizio Giordanetto1, Peter Nordberg1, Daniel Pettersen1, Nidhal Selmi1, Hans-Georg Beisel1, Hannah de la Motte1, Thomas Olsson1, Tim D J Perkins1, Margareta Herslöf1, Åsa Månsson1, Mikael Dahlström1, Ingemar Starke1, Johan Broddefalk1, Gabrielle Saarinen1, Fredrik Klingegård1, Eva Hurt-Camejo1, Birgitta Rosengren1, Johan Brengdahl2, Frank Jansen2, Mattias Rohman2, Jenny Sandmark2, Kenth Hallberg2, Tomas Åkerud2, Robert G Roth2, Marie Ahlqvist1.   

Abstract

In order to assess the potential of sPLA2-X as a therapeutic target for atherosclerosis, novel sPLA2 inhibitors with improved type X selectivity are required. To achieve the objective of identifying such compounds, we embarked on a lead generation effort that resulted in the identification of a novel series of indole-2-carboxamides as selective sPLA2-X inhibitors with excellent potential for further optimization.

Entities:  

Year:  2018        PMID： 30034585      PMCID： PMC6047051          DOI： 10.1021/acsmedchemlett.7b00505

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  20 in total

Review 1.  Phospholipase A2 enzymes and the risk of atherosclerosis.

Authors:  Robert S Rosenson; Eva Hurt-Camejo
Journal:  Eur Heart J       Date:  2012-07-15       Impact factor: 29.983

2.  Hydrolysis of lipoproteins by sPLA2's enhances mitogenesis and eicosanoid release from vascular smooth muscle cells: Diverse activity of sPLA2's IIA, V and X.

Authors:  Waldemar Pruzanski; Julia Kopilov; Arnis Kuksis
Journal:  Prostaglandins Other Lipid Mediat       Date:  2015-12-19       Impact factor: 3.072

3.  Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.

Authors:  S E Draheim; N J Bach; R D Dillard; D R Berry; D G Carlson; N Y Chirgadze; D K Clawson; L W Hartley; L M Johnson; N D Jones; E R McKinney; E D Mihelich; J L Olkowski; R W Schevitz; A C Smith; D W Snyder; C D Sommers; J P Wery
Journal:  J Med Chem       Date:  1996-12-20       Impact factor: 7.446

Review 4.  Varespladib methyl in cardiovascular disease.

Authors:  Robert S Rosenson; Heather Fraser; Joaquim Trias; Colin Hislop
Journal:  Expert Opin Investig Drugs       Date:  2010-10       Impact factor: 6.206

5.  Human group X secreted phospholipase A2 induces dendritic cell maturation through lipoprotein-dependent and -independent mechanisms.

Authors:  Rajai Atout; Sonia-Athina Karabina; Sandra Dollet; Martine Carreras; Christine Payré; Patrice André; Gérard Lambeau; Vincent Lotteau; Ewa Ninio; Laure Perrin-Cocon
Journal:  Atherosclerosis       Date:  2012-03-22       Impact factor: 5.162

6.  Crystal structure of human group X secreted phospholipase A2. Electrostatically neutral interfacial surface targets zwitterionic membranes.

Authors:  Ying H Pan; Bao-Zhu Yu; Alan G Singer; Farideh Ghomashchi; Gerard Lambeau; Michael H Gelb; Mahendra K Jain; Brian J Bahnson
Journal:  J Biol Chem       Date:  2002-05-25       Impact factor: 5.157

7.  Group V and X secretory phospholipase A(2)s-induced modification of high-density lipoprotein linked to the reduction of its antiatherogenic functions.

Authors:  Yoshikazu Ishimoto; Katsutoshi Yamada; Shigenori Yamamoto; Takashi Ono; Mitsuru Notoya; Kohji Hanasaki
Journal:  Biochim Biophys Acta       Date:  2003-10-21

8.  A flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones.

Authors:  Marc Nazaré; Claudia Schneider; Andreas Lindenschmidt; David William Will
Journal:  Angew Chem Int Ed Engl       Date:  2004-08-27       Impact factor: 15.336

Review 9.  Role of secretory phospholipases in atherogenesis.

Authors:  Ann-Cathrine Jönsson-Rylander; Sofia Lundin; Birgitta Rosengren; Camilla Pettersson; Eva Hurt-Camejo
Journal:  Curr Atheroscler Rep       Date:  2008-06       Impact factor: 5.113

10.  Varespladib and cardiovascular events in patients with an acute coronary syndrome: the VISTA-16 randomized clinical trial.

Authors:  Stephen J Nicholls; John J P Kastelein; Gregory G Schwartz; Dianna Bash; Robert S Rosenson; Matthew A Cavender; Danielle M Brennan; Wolfgang Koenig; J Wouter Jukema; Vijay Nambi; R Scott Wright; Venu Menon; A Michael Lincoff; Steven E Nissen
Journal:  JAMA       Date:  2014-01-15       Impact factor: 56.272
View more
  2 in total

1.  Design of Selective sPLA2-X Inhibitor (-)-2-{2-[Carbamoyl-6-(trifluoromethoxy)-1H-indol-1-yl]pyridine-2-yl}propanoic Acid.

Authors:  Fabrizio Giordanetto; Laurent Knerr; Peter Nordberg; Daniel Pettersen; Nidhal Selmi; Hans-Georg Beisel; Hannah de la Motte; Åsa Månsson; Mikael Dahlström; Johan Broddefalk; Gabrielle Saarinen; Fredrik Klingegård; Eva Hurt-Camejo; Birgitta Rosengren; Johannes Wikström; Maria Wågberg; Johan Brengdahl; Mattias Rohman; Jenny Sandmark; Tomas Åkerud; Robert G Roth; Frank Jansen; Marie Ahlqvist
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

Review 2.  Structural and Functional Aspects of Targeting the Secreted Human Group IIA Phospholipase A2.

Authors:  Ryung Rae Kim; Zheng Chen; Timothy J Mann; Karine Bastard; Kieran F Scott; W Bret Church
Journal:  Molecules       Date:  2020-09-28       Impact factor: 4.411
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.