Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors

[Display omitted] A series of furano[3,2-d]pyrimidine Syk inhibitors were synthesized and optimized for their enzyme potency and selectivity versus other kinases. In addition, ADME properties were assessed and compounds were prepared with optimized profiles for in vivo experiments. Compound 23 was i...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-11, Vol.26 (22), p.5562-5567
Hauptverfasser:	Hoemann, Michael, Wilson, Noel, Argiriadi, Maria, Banach, David, Burchat, Andrew, Calderwood, David, Clapham, Bruce, Cox, Phil, Duignan, David B., Konopacki, Don, Somal, Gagandeep, Vasudevan, Anil
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arthritis, Experimental - drug therapy Arthritis, Experimental - enzymology Dogs Furano[3,2-d]pyrimidine Furans - chemical synthesis Furans - chemistry Furans - pharmacology Furans - therapeutic use Humans Kinase inhibitor Molecular Docking Simulation Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Pyrimidines - chemistry Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Pyrimidines - therapeutic use Rats Rheumatoid arthritis Spleen tyrosine kinase Syk Syk Kinase - antagonists & inhibitors Syk Kinase - metabolism
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