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Bioorg Med Chem Lett. 2016 Nov 15;26(22):5562-5567. doi: 10.1016/j.bmcl.2016.09.077. Epub 2016 Oct 11.

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

Author information

1
AbbVie Bioresearch Center, 100 Research Dr., Worcester, MA 01545, United States.
2
AbbVie, 1 North Waukegan Rd., North Chicago, IL 60064, United States.
3
Reset Therapeutics, One Corporate Drive, South San Francisco, CA 94080, United States(†).

Abstract

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 identified as having acceptable pharmacokinetic properties and demonstrated efficacy in a rat collagen induced arthritis model.

KEYWORDS:

Furano[3,2-d]pyrimidine; Kinase inhibitor; Rheumatoid arthritis; Spleen tyrosine kinase; Syk

PMID:
27789138
DOI:
10.1016/j.bmcl.2016.09.077
[Indexed for MEDLINE]

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