Literature DB >> 17181139

Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators.

Rajeshwar Narlawar1, Blanca I Pérez Revuelta, Christian Haass, Harald Steiner, Boris Schmidt, Karlheinz Baumann.   

Abstract

N-sulfonylated and N-alkylated carprofen derivatives were investigated for their inhibition and modulation of gamma-secretase, which is associated with Alzheimer's disease. The introduction of a lipophilic substituent transformed the COX-2 inhibitor carprofen into a potent gamma-secretase modulator. Several compounds (e.g., 9p, 11f) caused selective reduction of Abeta42 and an increase of Abeta38. The most active compounds displayed activities in the low micromolar range and no effect on the gamma-secretase cleavage at the e-site.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 17181139     DOI： 10.1021/jm0610200

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

1.  Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.

Authors:  Isaac T Schiefer; Samer Abdul-Hay; Huali Wang; Michael Vanni; Zhihui Qin; Gregory R J Thatcher
Journal:  J Med Chem       Date:  2011-03-15       Impact factor: 7.446

2.  In Silico and Experimental Investigation of the Biological Potential of Some Recently Developed Carprofen Derivatives.

Authors:  Florea Dumitrascu; Ana-Maria Udrea; Mino R Caira; Diana Camelia Nuta; Carmen Limban; Mariana Carmen Chifiriuc; Marcela Popa; Coralia Bleotu; Anamaria Hanganu; Denisa Dumitrescu; Speranta Avram
Journal:  Molecules       Date:  2022-04-23       Impact factor: 4.927

3.  Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor.

Authors:  Angelo D Favia; Damien Habrant; Rita Scarpelli; Marco Migliore; Clara Albani; Sine Mandrup Bertozzi; Mauro Dionisi; Glauco Tarozzo; Daniele Piomelli; Andrea Cavalli; Marco De Vivo
Journal:  J Med Chem       Date:  2012-10-08       Impact factor: 7.446

4.  Substrate-targeting gamma-secretase modulators.

Authors:  Thomas L Kukar; Thomas B Ladd; Maralyssa A Bann; Patrick C Fraering; Rajeshwar Narlawar; Ghulam M Maharvi; Brent Healy; Robert Chapman; Alfred T Welzel; Robert W Price; Brenda Moore; Vijayaraghavan Rangachari; Bernadette Cusack; Jason Eriksen; Karen Jansen-West; Christophe Verbeeck; Debra Yager; Christopher Eckman; Wenjuan Ye; Sarah Sagi; Barbara A Cottrell; Justin Torpey; Terrone L Rosenberry; Abdul Fauq; Michael S Wolfe; Boris Schmidt; Dominic M Walsh; Edward H Koo; Todd E Golde
Journal:  Nature       Date:  2008-06-12       Impact factor: 49.962

Review 5.  Current pharmacotherapy and putative disease-modifying therapy for Alzheimer's disease.

Authors:  Akanksha Kulshreshtha; Poonam Piplani
Journal:  Neurol Sci       Date:  2016-06-01       Impact factor: 3.307

6.  Chemical Biology, Molecular Mechanism and Clinical Perspective of γ-Secretase Modulators in Alzheimer's Disease.

Authors:  Bruno Bulic; Julia Ness; Stefanie Hahn; Andreas Rennhack; Thorsten Jumpertz; Sascha Weggen
Journal:  Curr Neuropharmacol       Date:  2011-12       Impact factor: 7.363
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.