75129-09-8Relevant academic research and scientific papers
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
Agonists for the adenosine A1 receptor with tunable residence time. a case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines
Louvel, Julien,Guo, Dong,Agliardi, Marta,Mocking, Tamara A. M.,Kars, Roland,Pham, Tan Phát,Xia, Lizi,De Vries, Henk,Brussee, Johannes,Heitman, Laura H.,Ijzerman, Adriaan P.
supporting information, p. 3213 - 3222 (2014/05/20)
We report the synthesis and evaluation of previously unreported 4-amino-6-aryl-5-cyano-2-thiopyrimidines as selective human adenosine A 1 receptor (hA1AR) agonists with tunable binding kinetics, this without affecting their nanomolar affinity for the target receptor. They show a very diverse range of kinetic profiles (from 1 min (compound 52) to 1 h (compound 43)), and their structure-affinity relationships (SAR) and structure-kinetics relationships (SKR) were established. When put in perspective with the increasing importance of binding kinetics in drug discovery, these results bring new evidence of the consequences of affinity-only driven selection of drug candidates, that is, the potential elimination of slightly less active compounds that may display preferable binding kinetics.
Synthesis and antimicrobial activity of thioxopyrimidines and related derivatives
El-Agrody, Ahmed M.,Ali, Fawzy M.,Eid, Fathy A.,El-Nassag, Mohammed A. A.,El-Sherbeny, Gamal,Bedair, Ahmed H.
, p. 839 - 864 (2007/10/03)
The interaction of thiourea with activated cyanoolefins under different reaction conditions were studied, in which a variety of thiopyrimidines (8, 9, 12, 18, 20, & 21) and related derivatives (10, 11, 14, 16, & 17) were obtained respectively. Also, the r
A One Step Synthesis of New 4-Aminopyrimidine Derivatives: Preparation of Tetrazolo- and s-Triazolopyrimidines
Daboun, Hamed A.,El-Reedy, Ahmed M.
, p. 1686 - 1689 (2007/10/02)
2-Mercapto-4-amino-5-cyano-6-arylpyrimidines (1a, b), 2-hydroxy derivatives 1c, d and 2-methylmercapto derivatives 4a, b were synthesised via the reaction of either a mixture of malononitrile and aromatic aldehyde or arylidene malononitrile with thiourea,
