Delving into the Latest Updates on FCPE07 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

PDE4D

Mechanism

PDE4D inhibitors(phosphodiesterase 4D inhibitors)

Therapeutic Areas

Other Diseases

Active Indication

Depressive Disorder

Inactive Indication-

Originator Organization

Southern Medical University

Active Organization

Southern Medical University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC21H23F2NO4

InChIKeyDBNDIIUELFNMBG-UHFFFAOYSA-N

CAS Registry2033167-05-2

Depression involving neuroinflammation is one of the most common disabling and life-threatening psychiatric disorders. Phosphodiesterase 4 (PDE4) inhibitors produce potent antidepressant-like and cognition-enhancing effects. However, their clinical utility is limited by their major side effect of emesis. To obtain more selective PDE4 inhibitors with antidepressant and anti-neuroinflammation potential and less emesis, we designed and synthesized a series of N-alkyl catecholamides by modifying the 4-methoxybenzyl group of our hit compound, FCPE07, with an alkyl side chain. Among these compounds, 10 compounds displayed submicromolar IC₅₀ values in the mid- to low-nanomolar range. Moreover, 4-difluoromethoxybenzamides 10g and 10j, bearing isopropyl groups, exhibited the highest PDE4 inhibitory activities, with IC₅₀ values in the low-nanomolar range and with higher selectivities for PDE4 (approximately 5000-fold and 2100-fold over other PDEs, respectively). Furthermore, compound 10j displayed anti-neuroinflammation potential, promising antidepressant-like effects, and a zero incidence rate of emesis at 0.8 mg/kg within 180 min.

100 Deals associated with FCPE07

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