C. Hulme et al., QUATERNARY SUBSTITUTED PDE4 INHIBITORS I - THE SYNTHESIS AND IN-VITROEVALUATION OF A NOVEL SERIES OF OXINDOLES, Bioorganic & medicinal chemistry letters, 8(2), 1998, pp. 175-178
The following letter presents the synthesis and in vitro evaluation of
a novel quaternary substituted series of phosphodiesterase type (IV)
(PDE4) inhibitors. The compounds represent conformationally constraine
d analogues of the Celltech PDE IV inhibitor, CDP 840. Examples with s
ub-micromolar IC50's for PDE4 inhibition are reported. (C) 1998 Elsevi
er Science Ltd. All rights reserved.