Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0153470 (
Spleen
)
4,015
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The optimisation of the azanaphthyridine series of
Spleen
Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over hERG activity. A good pharmacokinetic profile was achieved by modification of the pKa. Morpholine compound 32 is a potent
SYK
inhibitor showing moderate selectivity, good oral bioavailability and good efficacy in the rat Arthus model but demonstrated a genotoxic potential in the Ames assay.
...
PMID:Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors. 2757 46
