65390-59-2

Usage

Molecular structure

Piperazine derivative with a 4-chlorophenoxy group and an ethyl chain attached to the piperazine ring

Potential use

Pharmaceutical intermediate

Pharmacological properties

Serotonin 5-HT1A receptor antagonist

Investigated for

Treatment of neurological and psychiatric disorders

Fields of interest

Medicinal chemistry and pharmacology

Biological activities

Potential biological activities due to its interaction with serotonin receptors

Pharmaceutical applications

Possible development of new drugs for the treatment of various disorders, based on its receptor antagonist properties

Upstream product

• 106-48-9 4-chloro-phenol 
• 110-85-0 piperazine 
• 2033-76-3 1-(2-bromoethoxy)-4-chlorobenzene 

Downstream Products

• 1352792-21-2 thiophen-2-yl(4-(2-(4-chlorophenoxy)ethyl)piperazin-1-yl)methanone 
• 1099242-60-0 (4-methoxyphenyl)(4-(2-(4-chlorophenoxy)ethyl)piperazin-1-yl)methanone 
• 1285857-96-6 N-phenyl-2-(4-(2-(4-chlorophenoxy)ethyl)piperazin-1-yl)acetamide 

Relevant academic research and scientific papers

Discovery of 1-aryloxyethyl piperazine derivatives as Kv1.5 potassium channel inhibitors (part I)

Kv1.5 potassium channel is an efficacious and safe therapeutic target for the treatment of atrial fibrillation (AF), the most common arrhythmia that threatens human. Herein, by modifying the hit compound 7k from an in-house database, 48 derivatives were synthesized for the assay of their Kv1.5 inhibitory effects by whole cell patch clamp technique. Six compounds which showed better potency than the positive compound dronedarone were selected for the next evaluation of their drug-like properties. Compound 8 exhibited balanced solubility and permeability. It also showed acceptable pharmacodynamics profile with very low acute toxicity. Taking all these data into account, compound 8 can serve as a promising lead for the development of novel therapeutic agent for the treatment of AF.