Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor† †Electronic supplementary information (ESI) available: Detailed experimental procedures and analytical characterisation of all compounds. See DOI: 10.1039/c7md00320j

@article{Fjellaksel2017SmallMP,
  title={Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor† †Electronic supplementary information (ESI) available: Detailed experimental procedures and analytical characterisation of all compounds. See DOI: 10.1039/c7md00320j},
  author={Richard Fjellaksel and Marc Boomgaren and R. Sundset and I. Haraldsen and J{\o}rn H Hansen and P. Riss},
  journal={MedChemComm},
  year={2017},
  volume={8},
  pages={1965 - 1969}
}
In this communication, we report the synthesis and characterization of a library of small molecule antagonists of the human gonadotropin releasing hormone receptor based upon the 2-(4-tert-butylphenyl)-4-piperazinyl-benzimidazole scaffold via Cu-catalysed azide alkyne cycloaddition. 
View PDF
5 Citations
Background Citations
1
Methods Citations
1

5 Citations

Citation Type

Citation Type

Recent Development of Non-Peptide GnRH Antagonists
  • 11
  • PDF
Discovery of a Lead Brain‐Penetrating Gonadotropin‐Releasing Hormone Receptor Antagonist with Saturable Binding in Brain
An acylation‐Finkelstein approach to radioiodination of bioactives: The role of amide group anchimeric assistance
  • 3
  • PDF
Evaluation by metabolic profiling and in vitro autoradiography of two promising GnRH-receptor ligands for brain SPECT imaging.
  • 1
First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
  • PDF

References

SHOWING 1-10 OF 19 REFERENCES
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
  • 23
Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
  • 9
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
  • 14
Effect of Testosterone Suppression on the Pharmacokinetics of a Potent GnRH Receptor Antagonist
  • 7
Drug Insight: clinical use of agonists and antagonists of luteinizing-hormone-releasing hormone
  • 139
Modulation of pharmacokinetics of radioiodinated sugar-conjugated somatostatin analogues by variation of peptide net charge and carbohydration chemistry.
  • 35
Testosterone surge: rationale for gonadotropin-releasing hormone blockers?
  • 92
Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers.
  • 14
Development of neuropeptide drugs that cross the blood-brain barrier
  • 96
  • PDF
Pharmacotherapy of paraphilias with long-acting agonists of luteinizing hormone-releasing hormone: a systematic review.
  • 113
...
1
2
...