Literature DB >> 21612933

New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis.

Virginie Andrzejak1, Giulio G Muccioli, Mathilde Body-Malapel, Jamal El Bakali, Madjid Djouina, Nicolas Renault, Philippe Chavatte, Pierre Desreumaux, Didier M Lambert, Régis Millet.   

Abstract

Growing evidence suggests a role for the endocannabinoid (EC) system, in intestinal inflammation and compounds inhibiting anandamide degradation offer a promising therapeutic option for the treatment of inflammatory bowel diseases. In this paper, we report the first series of carboxamides derivatives possessing FAAH inhibitory activities. Among them, compound 39 displayed significant inhibitory FAAH activity (IC(50)=0.088 μM) and reduced colitis induced by intrarectal administration of TNBS.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21612933     DOI: 10.1016/j.bmc.2011.04.057

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  8 in total

1.  Endocannabinoids Inhibit the Induction of Virulence in Enteric Pathogens.

Authors:  Melissa Ellermann; Alline R Pacheco; Angel G Jimenez; Regan M Russell; Santiago Cuesta; Aman Kumar; Wenhan Zhu; Gonçalo Vale; Sarah A Martin; Prithvi Raj; Jeffrey G McDonald; Sebastian E Winter; Vanessa Sperandio
Journal:  Cell       Date:  2020-10-07       Impact factor: 41.582

Review 2.  Cannabinoids for treating inflammatory bowel diseases: where are we and where do we go?

Authors:  Carina Hasenoehrl; Martin Storr; Rudolf Schicho
Journal:  Expert Rev Gastroenterol Hepatol       Date:  2017-02-16       Impact factor: 3.869

Review 3.  Cannabis, Cannabinoids, and the Endocannabinoid System-Is there Therapeutic Potential for Inflammatory Bowel Disease?

Authors:  Tim Ambrose; Alison Simmons
Journal:  J Crohns Colitis       Date:  2019-03-30       Impact factor: 9.071

4.  Use of Cannabinoids to Treat Acute Respiratory Distress Syndrome and Cytokine Storm Associated with Coronavirus Disease-2019.

Authors:  Prakash Nagarkatti; Kathryn Miranda; Mitzi Nagarkatti
Journal:  Front Pharmacol       Date:  2020-11-06       Impact factor: 5.810

5.  Synthesis, Physicochemical Characteristics and Plausible Mechanism of Action of an Immunosuppressive Isoxazolo[5,4-e]-1,2,4-Triazepine Derivative (RM33).

Authors:  Marcin Mączyński; Andrzej Regiec; Aleksandra Sochacka-Ćwikła; Iwona Kochanowska; Maja Kocięba; Ewa Zaczyńska; Jolanta Artym; Wojciech Kałas; Michał Zimecki
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-15

6.  Ethyl 5-(4-amino-phen-yl)isoxazole-3-carboxyl-ate.

Authors:  Jun-Tao Zhao; Jing-Jing Qi; You-Jun Zhou; Jia-Guo Lv; Ju Zhu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-17

Review 7.  Role of Cannabinoids in Gastrointestinal Mucosal Defense and Inflammation.

Authors:  Klára Gyires; Zoltán S Zádori
Journal:  Curr Neuropharmacol       Date:  2016       Impact factor: 7.363

Review 8.  Isoxazole Derivatives as Regulators of Immune Functions.

Authors:  Michał Zimecki; Urszula Bąchor; Marcin Mączyński
Journal:  Molecules       Date:  2018-10-22       Impact factor: 4.411

  8 in total

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