Fox DJ, Reckless J, Warren SG, Grainger DJ. (2002) Design, synthesis and preliminary pharmacological evaluation of N-alkyl 3-aminoglutarimides as broad spectrum chemokine inhibitors in vitro and anti-inflammatory agents in vivo. J. Med. Chem. 45:360-70
ABSTRACT: A series of N-substituted 3-aminoglutarimides have been synthesized and tested for inhibitory activity against a range of chemokines in vitro and for suppression of lipopolysaccharide-induced inflammation in vivo.
The results show that they represent the first class of small molecules with broad-spectrum chemokine inhibitory effects. Among the compounds studied, 10 (NR58,4) was the most potent, being active at doses between 5 and 15 nM in vitro and at 0.3 mg kg-1 in vivo.