296277-76-4Relevant academic research and scientific papers
Development of Covalent, Clickable Probes for Adenosine A1and A3Receptors
Trinh, Phuc N. H.,Chong, Daniel J. W.,Leach, Katie,Hill, Stephen J.,Tyndall, Joel D. A.,May, Lauren T.,Vernall, Andrea J.,Gregory, Karen J.
supporting information, p. 8161 - 8178 (2021/06/30)
Adenosine receptors are attractive therapeutic targets for multiple conditions, including ischemia-reperfusion injury and neuropathic pain. Adenosine receptor drug discovery efforts would be facilitated by the development of appropriate tools to assist in target validation and direct receptor visualization in different native environments. We report the development of the first bifunctional (chemoreactive and clickable) ligands for the adenosine A1receptor (A1R) and adenosine A3receptor (A3R) based on an orthosteric antagonist xanthine-based scaffold and on an existing structure-activity relationship. Bifunctional ligands were functional antagonists with nanomolar affinity and irreversible binding at the A1R and A3R. In-depth pharmacological profiling of these bifunctional ligands showed moderate selectivity over A2Aand A2Badenosine receptors. Once bound to the receptor, ligands were successfully “clicked” with a cyanine-5 fluorophore containing the complementary “click” partner, enabling receptor detection. These bifunctional ligands are expected to aid in the understanding of A1R and A3R localization and trafficking in native cells and living systems.
Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication
Kim, Junwon,Park, Changmin,Ok, Taedong,So, Wonyoung,Jo, Mina,Seo, Minjung,Kim, Youngmi,Sohn, Jeong-Hun,Park, Youngsam,Ju, Moon Kyeong,Kim, Junghwan,Han, Sung-Jun,Kim, Tae-Hee,Cechetto, Jonathan,Nam, Jiyoun,Sommer, Peter,No, Zaesung
scheme or table, p. 2119 - 2124 (2012/04/05)
3,4-Dihydropyrimidin-2(1H)-ones (DHPMs) were selected and derivatized through a HIV-1 replication assay based on GFP reporter cells. Compounds 14, 25, 31, and 36 exhibited significant inhibition of HIV-1 replication with a good safety profile. Chiral separation of each enantiomer by fractional crystallization showed that only the S enantiomer retained anti-HIV activity. Compound (S)-40, a novel and potent DHPM analog, could serve as an advanced lead for further development and the determination of the mechanism of action.
ANTI VIRAL COMPOUNDS
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Page/Page column 44-45, (2010/05/13)
There is provided small molecule anti-human immunodeficiency virus (anti-HIV) compounds as well as a phenotypic cell-based high throughput screening (HTS) assay for their identification.
Synthesis of the main metabolite in human blood of the A1 adenosine receptor ligand [18F]CPFPX
Holschbach, Marcus H.,Bier, Dirk,Wutz, Walter,Willbold, Sabine,Olsson, Ray A.
supporting information; experimental part, p. 4266 - 4269 (2009/12/28)
In human blood, the PET radiotracer [18F]CPFPX (1) Is metabolized to numerous metabolites, one (M1) being the most prominent in plasma 30 min p.i. Because the mass of injected tracer is ≤5 nmol, concentrations In plasma are too low to analyze.
