3HDZ: Identification, Synthesis, and SAR of Amino Substituted Pyrido[3,2b]pryaziones as Potent and Selective PDE5 Inhibitors

Citation:
Abstract
A new class of potent and selective PDE5 inhibitors is disclosed. Guided by X-ray crystallographic data, optimization of an HTS lead led to the discovery of a series of 2-aryl, (N8)-alkyl substituted-6-aminosubstituted pyrido[3,2b]pyrazinones which show potent inhibition of the PDE5 enzyme. Synthetic details and some structure-activity relationships are also presented.
PDB ID: 3HDZDownload
MMDB ID: 75172
PDB Deposition Date: 2009/5/7
Updated in MMDB: 2017/11
Experimental Method:
x-ray diffraction
Resolution: 1.8  Å
Source Organism:
Similar Structures:
Biological Unit for 3HDZ: monomeric; determined by author and by software (PISA)
Molecular Components in 3HDZ
Label Count Molecule
Protein (1 molecule)
1
Cgmp-specific 3',5'-cyclic Phosphodiesterase,camp-specific 3',5'-cyclic Phosphodiesterase 4a,cgmp-specific 3',5'-cyclic Phosphodiesterase
Molecule annotation
Chemicals (3 molecules)
1
1
2
1
3
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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