Development of benzodioxine-heteroarylpiperazines as highly potent and selective α2c antagonists

Bioorg Med Chem Lett. 2022 Dec 1:77:129005. doi: 10.1016/j.bmcl.2022.129005. Epub 2022 Sep 26.

Abstract

Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candidate molecules.

Keywords: (Benzodioxine); (Piperazine); (α2c Antagonist); α(2)-Adrenoceptors.

MeSH terms

  • Receptors, Adrenergic, alpha-2*

Substances

  • Receptors, Adrenergic, alpha-2