用于正电子发射断层扫描和单光子发射计算机断层扫描成像的突触囊泡蛋白2A（SV2A）配体的进一步研究：取代吡啶基甲基-4-（3,5-二氟苯基）吡咯烷-2-酮的合成与构效关系
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.
作者信息
Pracitto Richard, Wilcox Kyle C, Lindemann Marcel, Tong Jie, Zheng Chao, Li Songye, Finnema Sjoerd J, Huang Yiyun, Cai Zhengxin
机构信息
PET Center, Yale University School of Medicine, New Haven, Connecticut 06520, United States.
Translational Imaging Neuroscience, AbbVie, North Chicago, Illinois 60064, United States.
出版信息
ACS Omega. 2021 Oct 8;6(42):27676-27683. doi: 10.1021/acsomega.1c02433. eCollection 2021 Oct 26.
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.
合成了一系列突触小泡蛋白2A（SV2A）配体，以探索构效关系，并有助于进一步研究氢键药效团假说。以外消旋SynVesT-1作为先导化合物，探索用卤素和烃类取代吡啶基部分上的3-甲基。还研究了外消旋SynVesT-1的吡啶基异构体。发现了高效类似物，包括一种适合作为正电子发射断层扫描（PET）或单光子发射计算机断层扫描（SPECT）成像剂进行研究的3-碘吡啶基配体。
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