QUINAZOLINES - COMBINED TYPE-3 AND TYPE-4 PHOSPHODIESTERASE INHIBITORS

Authors
CHARPIOT B BRUN J DONZE I NAEF R STEFANI M MUELLER T
Citation
B. Charpiot et al., QUINAZOLINES - COMBINED TYPE-3 AND TYPE-4 PHOSPHODIESTERASE INHIBITORS, Bioorganic & medicinal chemistry letters, 8(20), 1998, pp. 2891-2896
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
20
Year of publication
1998
Pages
2891 - 2896
Database
ISI
SICI code
0960-894X(1998)8:20<2891:Q-CTAT>2.0.ZU;2-Q
Abstract
A series of quinazolines has been prepared and evaluated for its abili ty to inhibit cyclic AMP phosphodiesterase type 3, type 4A, 4B and 4D. The most potent inhibitors showed IC50 values in the nanomolar range far type 3 and type 4 isoforms and bind with high affinity to the [H-3 ]rolipram binding site. These quinazolines represent a new family of p otent mixed PDE 3 / 4 inhibitors and are expected to have a therapeuti c potential. (C) 1998 Elsevier Science Ltd. All rights reserved.