917758-83-9Relevant academic research and scientific papers
Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase
De Jonghe, Steven,Einav, Shirit,Froeyen, Mathy,Herdewijn, Piet,Martinez-Gualda, Belén,Pu, Szu-Yuan
, (2019/12/24)
Previously, we reported the discovery of 3,6-disubstituted isothiazolo[4,3-b]pyridines as potent and selective cyclin G-associated kinase (GAK) inhibitors with promising antiviral activity. In this manuscript, the structure-activity relationship study was expanded to synthesis of isothiazolo[4,3-b]pyridines with modifications of the pyridine moiety. This effort led to the discovery of an isothiazolo[4,3-b]pyridine derivative with a 3,4-dimethoxyphenyl residue at position 5 that displayed low nanomolar GAK binding affinity and antiviral activity against dengue virus.
Optimization of pharmacokinetics through manipulation of physicochemical properties in a series of HCV inhibitors
Lazerwith, Scott E.,Bahador, Gina,Canales, Eda,Cheng, Guofeng,Chong, Lee,Clarke, Michael O.,Doerffler, Edward,Eisenberg, Eugene J.,Hayes, Jaclyn,Lu, Bing,Liu, Qi,Matles, Mike,Mertzman, Michael,Mitchell, Michael L.,Morganelli, Philip,Murray, Bernard P.,Robinson, Margaret,Strickley, Robert G.,Tessler, Megan,Tirunagari, Neeraj,Wang, Jianhong,Wang, Yujin,Zhang, Jennifer R.,Zheng, Xubin,Zhong, Weidong,Watkins, William J.
supporting information; experimental part, p. 715 - 719 (2011/12/01)
A novel series of HCV replication inhibitors based on a pyrido[3,2-d]pyrimidine core were optimized for pharmacokinetics (PK) in rats. Several associations between physicochemical properties and PK were identified and exploited to guide the design of comp
2,4,6-TRISUBSTITUTED PYRIDO (3,2-d) PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS
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Page/Page column 70, (2010/04/03)
Pyrido(3,2-d)pyrimidine derivatives represented by the structural formuia (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro
PYRIDO(3,2-D)PYRIMIDINES USEFUL FOR TREATING VIRAL INFECTIONS
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Page/Page column 55-56, (2008/12/06)
Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salt
