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5-HT6 receptor antagonists. Design, synthesis, and structure-activity relationship of substituted 2-(1-methyl-4-piperazinyl)pyridines

In this study, we present the discovery and pharmacological characterization of a new series of 6-piperazinyl-7-azaindoles. These compounds demonstrate potent antagonism and selectivity against the 5-HT6 receptor. Our research primarily focuses on optimizing the lead structure and investigating the structure-activity relationship (SAR) of these compounds. Our main objective is to improve their activity and selectivity against off-target receptors. Overall, our findings contribute to the advancement of novel compounds targeting the 5-HT6 receptor. Compound 29 exhibits significant promise in terms of pharmacological, physicochemical, and ADME (Absorption, Distribution, Metabolism, and Excretion) properties. Consequently, it merits thorough exploration as a potential drug candidate due to its favorable activity profile and successful outcomes in a range of in vivo experiments.

 

Comments:

It sounds like you're describing a research study focused on the discovery and characterization of a new series of compounds with potential pharmaceutical applications. In this study, the researchers have identified a group of 6-piperazinyl-7-azaindoles that show potent antagonistic effects specifically against the 5-HT6 receptor, demonstrating selectivity for this receptor over other off-target receptors.

The primary goals of the research include optimizing the lead structure and understanding the structure-activity relationship (SAR) of these compounds. By doing so, the researchers aim to enhance the compounds' activity and selectivity against receptors other than the 5-HT6 receptor. This is a crucial step in drug development, as it helps in minimizing potential side effects and maximizing therapeutic efficacy.

Compound 29 has been highlighted as particularly promising due to its favorable pharmacological, physicochemical, and ADME (Absorption, Distribution, Metabolism, and Excretion) properties. It has shown positive results in various in vivo experiments, suggesting its potential as a drug candidate. Further research and exploration of this compound are recommended to determine its viability as a pharmaceutical agent.

Related Products

Cat.No. Product Name Information
S6636 Azaindole 1 (BAY-549) Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.

Related Targets

ROCK