5468-91-7

Usage

Class

Phenylpropanoic acids

Usage

Non-steroidal anti-inflammatory drug (NSAID)

Effects

Analgesic and anti-inflammatory

Mechanism of action

Inhibits the production of prostaglandins responsible for inflammation and pain

Potential applications

Cancer treatment and prevention, management of neurodegenerative disorders

Promising for

Further research and development in pharmaceuticals and medicinal chemistry

Upstream product

• 2958-56-7 2‐(3,4‐dimethoxyphenyl)‐3‐phenylpropanenitrile 
• 93-17-4 3,4-dimethoxyphenylacetonitrile 

Relevant academic research and scientific papers

Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design

Alzheimer's disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor 1, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogues, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational analysis of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.

GUANIDINE DERIVATIVES AS TRPC MODULATORS

The present invention is directed to guanidine derivatives as inhibitors of transient receptor potential canonical channels (TRPC channels), in particular TRPC3 and/or TRPC6 and/or TRPC7 activity, more particularly TRPC6 activity. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by TRPC channels (Formula (I))