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4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis.
J Med Chem. 2012 Oct 25; 55(20):8948-52.JM

Abstract

Further on to our earlier work on the 4-oxo-1,4-dihydropyridine, we describe herein our strategy to get access to potent selective CB2 receptor agonists. Thus, we designed and synthesized 29 compounds, evaluated on both hCB1 and hCB2 cannabinoid receptors, and assessed 11 of them in the TNBS-induced colitis model in mice. Compound 48 was found to be the most efficient of our series, exhibiting an exquisite protection against experimental colitis, superior to the one observed after treatment with Pentasa.

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Publisher Full Text (DOI)

Authors+Show Affiliations

El Bakali J
ICPAL, Université Lille Nord de France , EA4481, IFR114, 3 Rue du Pr. Laguesse, BP 83, F-59006 Lille Cedex, France.
Gilleron P
No affiliation info available
Body-Malapel M
No affiliation info available
Mansouri R
No affiliation info available
Muccioli GG
No affiliation info available
Djouina M
No affiliation info available
Barczyk A
No affiliation info available
Klupsch F
No affiliation info available
Andrzejak V
No affiliation info available
Lipka E
No affiliation info available
Furman C
No affiliation info available
Lambert DM
No affiliation info available
Chavatte P
No affiliation info available
Desreumaux P
No affiliation info available
Millet R
No affiliation info available

MeSH

AdamantaneAnimalsAnti-Inflammatory Agents, Non-SteroidalBinding, CompetitiveBlood ProteinsCHO CellsColitisCricetinaeCricetulusHumansIntestinal AbsorptionLigandsMiceMicrosomes, LiverProtein BindingPyridinesRadioligand AssayReceptor, Cannabinoid, CB2Structure-Activity RelationshipTrinitrobenzenesulfonic Acid

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23017078

Citation

El Bakali, Jamal, et al. "4-Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands. Part 2: Discovery of New Agonists Endowed With Protective Effect Against Experimental Colitis." Journal of Medicinal Chemistry, vol. 55, no. 20, 2012, pp. 8948-52.
El Bakali J, Gilleron P, Body-Malapel M, et al. 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. J Med Chem. 2012;55(20):8948-52.
El Bakali, J., Gilleron, P., Body-Malapel, M., Mansouri, R., Muccioli, G. G., Djouina, M., Barczyk, A., Klupsch, F., Andrzejak, V., Lipka, E., Furman, C., Lambert, D. M., Chavatte, P., Desreumaux, P., & Millet, R. (2012). 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. Journal of Medicinal Chemistry, 55(20), 8948-52. https://doi.org/10.1021/jm3008568
El Bakali J, et al. 4-Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands. Part 2: Discovery of New Agonists Endowed With Protective Effect Against Experimental Colitis. J Med Chem. 2012 Oct 25;55(20):8948-52. PubMed PMID: 23017078.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis. AU - El Bakali,Jamal, AU - Gilleron,Pauline, AU - Body-Malapel,Mathilde, AU - Mansouri,Roxane, AU - Muccioli,Giulio G, AU - Djouina,Madjid, AU - Barczyk,Amélie, AU - Klupsch,Frédérique, AU - Andrzejak,Virginie, AU - Lipka,Emmanuelle, AU - Furman,Christophe, AU - Lambert,Didier M, AU - Chavatte,Philippe, AU - Desreumaux,Pierre, AU - Millet,Régis, Y1 - 2012/10/12/ PY - 2012/9/29/entrez PY - 2012/9/29/pubmed PY - 2013/2/6/medline SP - 8948 EP - 52 JF - Journal of medicinal chemistry JO - J Med Chem VL - 55 IS - 20 N2 - Further on to our earlier work on the 4-oxo-1,4-dihydropyridine, we describe herein our strategy to get access to potent selective CB2 receptor agonists. Thus, we designed and synthesized 29 compounds, evaluated on both hCB1 and hCB2 cannabinoid receptors, and assessed 11 of them in the TNBS-induced colitis model in mice. Compound 48 was found to be the most efficient of our series, exhibiting an exquisite protection against experimental colitis, superior to the one observed after treatment with Pentasa. SN - 1520-4804 UR - https://www.unboundmedicine.com/medline/citation/23017078/4_Oxo_14_dihydropyridines_as_selective_CB2_cannabinoid_receptor_ligands__Part_2:_discovery_of_new_agonists_endowed_with_protective_effect_against_experimental_colitis_ DB - PRIME DP - Unbound Medicine ER -