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Bioorg Med Chem Lett. 2014 Oct 1;24(19):4759-4762. doi: 10.1016/j.bmcl.2014.07.048. Epub 2014 Aug 14.

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

Author information

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.

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

PMID:
25182564
PMCID:
PMC4294696
DOI:
10.1016/j.bmcl.2014.07.048
[Indexed for MEDLINE]
Free PMC Article

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