2. Academic Validation
  3. Synthesis and evaluation of arylpiperazines derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands

Synthesis and evaluation of arylpiperazines derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands

  • Bioorg Med Chem Lett. 2014 Oct 1;24(19):4759-4762. doi: 10.1016/j.bmcl.2014.07.048.
J S Dileep Kumar 1,  Vattoly J Majo 2,  Jaya Prabhakaran 3,  J John Mann 4
Affiliations

Affiliations

  • 1 Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA; Department of Psychiatry and Behavior Science, Stony Brook University, New York, USA. Electronic address: kumardi@nyspi.columbia.edu.
  • 2 Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA.
  • 3 Columbia University College of Physicians and Surgeons, New York, USA.
  • 4 Division of Molecular Imaging and Neuropathology, New York State Psychiatric Institute, New York, USA; Columbia University College of Physicians and Surgeons, New York, USA.
PMID: 25182564 DOI: 10.1016/j.bmcl.2014.07.048
Abstract

5-HT1AR agonist or partial agonists are established drug candidates for psychiatric and neurological disorders. We have reported the synthesis and evaluation of a series of high affinity 5-HT1AR partial agonist PET imaging agents with greater selectivity over α-1AR. The characteristic of these molecules are 3,5-dioxo-(2H,4H)-1,2,4-triazine skeleton tethered to an arylpiperazine unit through an alkyl side chain. The most potent 5-HT1AR agonistic properties were found to be associated with the molecules bearing C-4 alkyl group as the linker. Therefore development of 3,5-dioxo-(2H,4H)-1,2,4-triazine bearing arylpiperazine derivatives may provide high affinity selective 5-HT1AR ligands. Herein we describe the synthesis and evaluation of the binding properties of a series of arylpiperazine analogues of 3,5-dioxo-(2H,4H)-1,2,4-triazine.

Keywords

5-HT; 5-HT(1A)R; Agonist; Arylpiperazine; α-1AR.

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