Further Investigation of Synaptic Vesicle Protein 2A (SV2A) Ligands Designed for Positron Emission Tomography and Single-Photon Emission Computed Tomography Imaging: Synthesis and Structure–Activity Relationship of Substituted Pyridinylmethyl-4-(3,5-difluorophenyl)pyrrolidin-2-ones

[Image: see text] A series of synaptic vesicle protein 2A (SV2A) ligands were synthesized to explore the structure–activity relationship and to help further investigate a hydrogen bonding pharmacophore hypothesis. Racemic SynVesT-1 was used as a lead compound to explore the replacement of the 3-meth...

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Detalles Bibliográficos
Autores principales: Pracitto, Richard, Wilcox, Kyle C., Lindemann, Marcel, Tong, Jie, Zheng, Chao, Li, Songye, Finnema, Sjoerd J., Huang, Yiyun, Cai, Zhengxin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8552234/
https://www.ncbi.nlm.nih.gov/pubmed/34722967
http://dx.doi.org/10.1021/acsomega.1c02433
Descripción
Sumario:[Image: see text] A series of synaptic vesicle protein 2A (SV2A) ligands were synthesized to explore the structure–activity relationship and to help further investigate a hydrogen bonding pharmacophore hypothesis. Racemic SynVesT-1 was used as a lead compound to explore the replacement of the 3-methyl group on the pyridinyl moiety with halogens and hydrocarbons. Pyridinyl isomers of racemic SynVesT-1 were also investigated. Highly potent analogs were discovered including a 3-iodo pyridinyl ligand amenable to investigation as a PET or SPECT imaging agent.

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