Delving into the Latest Updates on PDE7A inhibitors(Emory University) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Compound 26(Emory University)

Target

PDE7A

Action

inhibitors

Mechanism

PDE7A inhibitors(phosphodiesterase 7A inhibitors)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

InflammationNeurodegenerative Diseases

Inactive Indication-

Originator Organization

Emory University

Active Organization

Emory University

Inactive Organization-

License Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC25H26ClN5O2

InChIKeyHHARCTVDZIAPSF-LJQANCHMSA-N

CAS Registry3074559-75-1

Phosphodiesterases (PDEs) have drawn attention due to their critical roles in physiological and pathological conditions. Many research groups have studied these hydrolytic enzymes to develop new drugs, including apremilast as a PDE4 inhibitor and sildenafil as a PDE5 inhibitor. Targeting PDE7 has also been deemed a rational strategy to ameliorate autoimmune conditions. However, to date, no successful clinical results have been reported. We postulated that progress in these studies with PDE7 had been hampered by the lack of a potent ligand with a reasonable selectivity for this PDE isozyme. Therefore, starting from a PDE7A/7B dual inhibitor, our investigations led to improved selectivity along with extended metabolic stability, resulting in a novel PDE7A inhibitor 26. This compound with high selectivity over the closest isozyme is an ideal chemical entity to unveil new pharmacological roles of PDE7A-dependent signaling, as exemplified by the in vivo antiosteoporotic effects.

100 Deals associated with PDE7A inhibitors(Emory University)

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