Literature DB >> 18289847

Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).

Amy Timmons1, Mark Seierstad, Rich Apodaca, Matt Epperson, Dan Pippel, Sean Brown, Leon Chang, Brian Scott, Michael Webb, Sandra R Chaplan, J Guy Breitenbucher.   

Abstract

Efforts to improve the properties of the well studied ketooxazole FAAH inhibitor OL-135 resulted in the discovery of a novel propylpiperidine series of FAAH inhibitors that has a modular design and superior properties to OL-135. The efficacy of one of these compounds was demonstrated in a rat spinal nerve ligation model of neuropathic pain in rats.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18289847     DOI： 10.1016/j.bmcl.2008.01.091

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


  9 in total

Review 1.  The case for the development of novel analgesic agents targeting both fatty acid amide hydrolase and either cyclooxygenase or TRPV1.

Authors:  C J Fowler; P S Naidu; A Lichtman; V Onnis
Journal:  Br J Pharmacol       Date:  2009-02       Impact factor: 8.739

Review 2.  The endocannabinoid system and pain.

Authors:  Josée Guindon; Andrea G Hohmann
Journal:  CNS Neurol Disord Drug Targets       Date:  2009-12       Impact factor: 4.388

Review 3.  The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).

Authors:  Katerina Otrubova; Cyrine Ezzili; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2011-06-28       Impact factor: 2.823

4.  Fatty acid amide hydrolase as a potential therapeutic target for the treatment of pain and CNS disorders.

Authors:  Kay Ahn; Douglas S Johnson; Benjamin F Cravatt
Journal:  Expert Opin Drug Discov       Date:  2009-07       Impact factor: 6.098

5.  Fluoride-mediated capture of a noncovalent bound state of a reversible covalent enzyme inhibitor: X-ray crystallographic analysis of an exceptionally potent α-ketoheterocycle inhibitor of fatty acid amide hydrolase.

Authors:  Mauro Mileni; Joie Garfunkle; Cyrine Ezzili; Benjamin F Cravatt; Raymond C Stevens; Dale L Boger
Journal:  J Am Chem Soc       Date:  2011-02-28       Impact factor: 15.419

Review 6.  On the Biomedical Properties of Endocannabinoid Degradation and Reuptake Inhibitors: Pre-clinical and Clinical Evidence.

Authors:  Karen Jaqueline Paredes-Ruiz; Karla Chavira-Ramos; Mario Orozco-Morales; Cimen Karasu; Alexey A Tinkov; Michael Aschner; Abel Santamaría; Ana Laura Colín-González
Journal:  Neurotox Res       Date:  2021-11-06       Impact factor: 3.911

7.  A copper-catalyzed, pH-neutral construction of high-enantiopurity peptidyl ketones from peptidic s-acylthiosalicylamides in air at room temperature.

Authors:  Lanny S Liebeskind; Hao Yang; Hao Li
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336

8.  X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.

Authors:  Mauro Mileni; Joie Garfunkle; Cyrine Ezzili; F Scott Kimball; Benjamin F Cravatt; Raymond C Stevens; Dale L Boger
Journal:  J Med Chem       Date:  2010-01-14       Impact factor: 7.446

9.  Synthesis of high enantiopurity N-protected alpha-amino ketones by thiol ester-organostannane cross-coupling using pH-neutral conditions.

Authors:  Hao Li; Hao Yang; Lanny S Liebeskind
Journal:  Org Lett       Date:  2008-08-30       Impact factor: 6.005
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.