Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities

Francis Giraud; Pascal Marchand; Delphine Carbonnelle; Michael Sartor; François Lang; Muriel Duflos

doi:10.1016/j.bmcl.2010.07.001

Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5203-6. doi: 10.1016/j.bmcl.2010.07.001. Epub 2010 Jul 6.

Authors

Francis Giraud¹, Pascal Marchand, Delphine Carbonnelle, Michael Sartor, François Lang, Muriel Duflos

Affiliation

¹ Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections, de l'Immunité et du Cancer, IICiMed UPRES EA 1155, Faculté de Pharmacie, Nantes, France.

PMID: 20655209
DOI: 10.1016/j.bmcl.2010.07.001

Abstract

N-aryl-3-(indol-3-yl)propanamides were synthesized and their immunosuppressive activities were evaluated. This study highlighted the promising potency of 3-[1-(4-chlorobenzyl)-1H-indol-3-yl]-N-(4-nitrophenyl)propanamide 15 which exhibited a significant inhibitory activity on murine splenocytes proliferation assay in vitro and on mice delayed-type hypersensitivity (DTH) assay in vivo.

MeSH terms

Amides / chemical synthesis*
Amides / pharmacology*
Animals
Hypersensitivity, Delayed
Immunosuppressive Agents / chemical synthesis*
Immunosuppressive Agents / pharmacology*
In Vitro Techniques
Indoles / chemistry
Inhibitory Concentration 50
Mice

Substances

Amides
Immunosuppressive Agents
Indoles