735273-35-5Relevant academic research and scientific papers
Discovery of Highly Potent Adenosine A1Receptor Agonists: Targeting Positron Emission Tomography Probes
Bakhoda, Abolghasem,Eisenberg, Seth M.,Fowler, Joanna S.,Gao, Zhan-Guo,Guo, Min,Hooker, Jacob M.,Jacobson, Kenneth A.,Javdan, Cameron,Kang, Yeona,Kelleher, Andrew C.,Kim, Sung Won,Li, Yang,O'Conor, Kelly A.,Ramsey, Joseph M.,Rice, Kenner C.,Volkow, Nora D.,Yan, Xuefeng
, (2021/09/27)
Adenosine receptor (AR) radiotracers for positron emission tomography (PET) have provided knowledge on the in vivo biodistribution of ARs in the central nervous system (CNS), which is of therapeutic interest for various neuropsychiatric disorders. Additio
Preclinical Evaluation of the First Adenosine A1 Receptor Partial Agonist Radioligand for Positron Emission Tomography Imaging
Guo, Min,Gao, Zhan-Guo,Tyler, Ryan,Stodden, Tyler,Li, Yang,Ramsey, Joseph,Zhao, Wen-Jing,Wang, Gene-Jack,Wiers, Corinde E.,Fowler, Joanna S.,Rice, Kenner C.,Jacobson, Kenneth A.,Kim, Sung Won,Volkow, Nora D.
, p. 9966 - 9975 (2018/11/23)
Central adenosine A1 receptor (A1R) is implicated in pain, sleep, substance use disorders, and neurodegenerative diseases, and is an important target for pharmaceutical development. Radiotracers for A1R positron emission t
Library design, synthesis, and screening: Pyridine dicarbonitriles as potential prion disease therapeutics
Reddy, Tummala R. K.,Mutter, Roger,Heal, William,Guo, Kai,Gillet, Valerie J.,Pratt, Steven,Chen, Beining
, p. 607 - 615 (2007/10/03)
Transmissible spongiform encephalopathies (TSEs) or prion diseases are a family of invariably fatal neurodegenerative disorders, and there are no effective therapeutics currently available. In this paper, we report on the design, synthesis, and screening of a series of pyridine dicarbonitriles as potential novel prion disease therapeutics. A virtual reaction-based library of 1050 compounds was constructed. Docking and evaluation using GOLD scores assisted the initial selection of compounds for synthesis. The selection was augmented with further compounds to increase structural diversity. A total of 45 compounds were synthesized via a one-pot three-component coupling reaction. The mechanism of the three-component coupling reaction was investigated, and it was discovered that chemical oxidation is required for the last step, forming the pyridine ring (aromatization). A total of 19 compounds were identified as binders to one or more forms of prion protein by in vitro screening using surface plasmon resonance (SPR). A selection of compounds were investigated for activity in cells, resulting in the discovery of a new inhibitor of PrP Sc formation.
New, non-adenosine, high-potency agonists for the human adenosine A 2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine
Beukers, Margot W.,Chang, Lisa C. W.,Von Frijtag Drabbe Künzel, Jacobien K.,Mulder-Krieger, Thea,Spanjersberg, Ronald F.,Brussee, Johannes,Ijzerman, Ad P.
, p. 3707 - 3709 (2007/10/03)
The adenosine A2B receptor is the least well characterized of the four known adenosine receptor subtypes because of the absence of potent, selective agonists. Here, we present five non-adenosine agonists. Among them, 2-amino-4-(4-hydroxyphenyl)
