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 Rune Sundset and Ira H. Haraldsen and J{\o}rn H. Hansen and Patrick Johannes 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.
6 Citations
Recent Development of Non-Peptide GnRH Antagonists
- BiologyMolecules
- 2017
All developed small molecule GnRH antagonists are summarized along with the most recent clinical data and therapeutic applications for hormone-dependent diseases targeting the GnRH receptor.
Discovery of a Lead Brain‐Penetrating Gonadotropin‐Releasing Hormone Receptor Antagonist with Saturable Binding in Brain
- Biology, ChemistryChemMedChem
- 2020
Positron emission tomography imaging in rat under baseline conditions in comparison to pretreatment with a receptor‐saturating dose of GnRH antagonist revealed saturable uptake into the brain.
A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives
- Chemistry, BiologyFrontiers in Pharmacology
- 2021
This comprehensive review has summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship.
An acylation‐Finkelstein approach to radioiodination of bioactives: The role of amide group anchimeric assistance
- Chemistry, Biology
- 2018
A straightforward sequential acylation-Finkelstein approach to achieve iodination of amine containing bioactives and discloses a number of fundamental aspects of amide group anchimeric assistance in substitution reactions.
Evaluation by metabolic profiling and in vitro autoradiography of two promising GnRH-receptor ligands for brain SPECT imaging.
- Biology, ChemistryJournal of labelled compounds & radiopharmaceuticals
- 2019
A preclinical evaluation of the compound properties was performed to evaluate their potential as Single Photon Emission Computed Tomography (SPECT) radiotracers for imaging the GnRH-receptor and found that compounds 3 and 4 binds to rat Gn RH-R in different rat brain regions.
First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor
- BiologyBMC research notes
- 2018
The compound was found to possess nano molar affinity for the gonadotropin releasing hormone-receptor in a competition dependent inhibition study and liquid chromatography-mass spectrometry analysis in saline, human and rat serum resulted in 46%, 52% and 44% stability after incubation for 1 h respectively.
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