124953-38-4

Usage

Chemical class

Piperazine derivative

Structural features

Contains an isoxazole ring
Contains a carbonyl group attached to the piperazine moiety
5-methyl-3-phenyl substitution on the isoxazole ring

Potential applications

Psychoactive drug
Medicinal chemistry
Drug development

Pharmacological properties

Studied for its potential effects on the central nervous system

Research interest

Due to its unique structure and potential applications, it is a molecule of interest for further research and potential pharmaceutical use.

Upstream product

• 16883-16-2 5-methyl-3-phenylisoxazole-4-carbonyl chloride 
• 59813-07-9 piperazine monohydrobromide 

Downstream Products

• 124953-47-5 4-(5-Methyl-3-phenyl-isoxazole-4-carbonyl)-piperazine-1-carbothioic acid (2-cyano-4,5-dimethoxy-phenyl)-amide 

Relevant academic research and scientific papers

New isoxazole derivatives provided with antihypertensive activity

A series of diazacycloalkane-quinazoline derivatives of isoxazoles were synthesized and tested in order to identify new potent and selective α1-antagonists. A preliminary screening by using in vitro tests such as binding assay (3H-prazosin and 3H-rauwolscine displacement) and analysis of antagonistic activity in isolated rat aorta (norepinephrine-induced response) and in isolated rat vas deferens (clonidine-induced response) indicated that many of these compounds exhibited a good affinity and selectivity towards α1-adrenergic receptors associated with potent pharmacological activity. In particular, a 3-bromo-5-isoxazolecarbonyl derivative, selected for further in vivo investigation, was provided with as high antihypertensive action as prazosin in spontaneously hypertensive rats (SHR) coupled to a shallow dose-response curve by route. Moreover, a higher ratio between oral antihypertensive dosis in SHR and normotensive rats was found with respect to reference compound prazosin.