208254-23-3Relevant 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
4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents
Alder, Arne,Gilberger, Tim,Kunick, Conrad,Schwed, Sandra I.
, (2020/08/24)
Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-b]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions. In contrast to the related ketones, these carboxamides are only weak inhibitors of the plasmodial enzyme PfGSK-3 but the compounds nevertheless show strong antiparasitic activity. The most potent representatives inhibit the pathogens with IC50values in the two-digit nanomolar range and exhibit high selectivity indices (>100).
SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF
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Paragraph 0412-0415, (2013/08/28)
The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor
Chang, Lisa C. W.,Von Frijtag Drabbe Künzel, Jacobien K.,Mulder-Krieger, Thea,Spanjersberg, Ronald F.,Roerink, Sophie F.,Van Den Hout, Gijs,Beukers, Margot W.,Brussee, Johannes,Ijzerman, Adriaan P.
, p. 2045 - 2053 (2007/10/03)
Adenosine receptor agonists are usually variations of the natural ligand, adenosine. The ribose moiety in the ligand has previously been shown to be of great importance for the agonistic effects of the compound. In this paper, we present a series of nonadenosine ligands selective for the adenosine A 1 receptor with an extraordinary pharmacological profile. 2-Amino-4-benzo-[1,3]dioxol-5-yl-6-(2-hydroxyethylsulfanyl)pyridine-3, 5-dicarbonitrile (70, LUF 5853) shows full agonistic behavior comparable with the reference compound CPA, while also displaying comparable receptor binding affinity (Ki = 11 nM). In contrast, compound 58 (2-amino-4-(3- trifluoromethylphenyl)-6-(2-hydroxyethylsulfanyl)pyridine-3,5-dicarbonitrile, LUF 5948) has a binding affinity of 14 nM and acts as an inverse agonist. Also present within this same series are compounds that show neutral antagonism of the adenosine A1 receptor, for example compound 65 (2-amino-4-(4-difluoromethoxyphenyl)-6-(2-hydroxyethylsulfanyl)pyridine-3, 5-dicarbonitrile, LUF 5826).
New Route to 6-Amino-4-aryl-3,5-dicyano-pyridine-2(1H)-thiones
Dyachenko,Krivokolysko,Sharanin,Litvinov
, p. 1014 - 1017 (2007/10/03)
Condensation of aromatic aldehydes with a twofold amount of cyanothioacetamide yields 6-amino-4-aryl-3,5-dicyanopyridine-2(1H)-thiones. These compounds are also formed by recyclization of 2,6-diamino-4-aryl-3,5-dicyano-4H-thiopyrans. 6-Amino-4-aryl-3,5-dicyanopyridine-2(1H)-thiones were used to prepare substituted 2-alkylthiopyridines and thieno[2,3-6]pyridines.
