| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596855 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
The synthesis and SAR of tetracyclic MK2 inhibitors is reported. Spirocyclopropyl- and spiroazetidine groups attached to the δ-ring produced potent MK2-inhibitors with oral activity in the acute LPS-induced TNFα release model in mice. Compound 13E showed significant reduction of swelling and histological scores in two chronic arthritis models upon oral administration.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Laszlo Revesz, Achim Schlapbach, Reiner Aichholz, Janet Dawson, Roland Feifel, Stuart Hawtin, Amanda Littlewood-Evans, Guido Koch, Markus Kroemer, Henrik Möbitz, Clemens Scheufler, Juraj Velcicky, Christine Huppertz,