GNF6702

GNF6702
Identifiers
	IUPAC name N-[4-fluoro-3-(6-pyridin-2-yl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)phenyl]-2,4-dimethyl-1,3-oxazole-5-carboxamide;
CAS Number	1799329-72-8 ;
PubChem CID	91810392;
ChemSpider	58827646;
UNII	9NKU4X5ZKZ;
ChEBI	CHEBI:133824 ;
CompTox Dashboard (EPA)	DTXSID201336032 ;
Chemical and physical data
Formula	C22H16FN7O3
Molar mass	445.414 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES n5ccccc5-c(cn1n4)cnc1nc4-c3cc(ccc3F)NC(=O)c2oc(C)nc2C;
	InChI InChI=1S/C22H16FN7O2/c1-12-19(32-13(2)26-12)21(31)27-15-6-7-17(23)16(9-15)20-28-22-25-10-14(11-30(22)29-20)18-5-3-4-8-24-18/h3-11H,1-2H3,(H,27,31); Key:WXZFCGRYVWYYTG-UHFFFAOYSA-N;

GNF6702 is the name for a broad-spectrum antiprotozoal drug invented by researchers working at the Genomics Institute of the Novartis Research Foundation in 2013,^[1] with activity against leishmaniasis, Chagas disease and sleeping sickness. These three diseases are caused by related kinetoplastid parasites, which share similar biology. GNF6702 acts as allosteric proteasome inhibitor which was effective against infection with any of the three protozoal diseases in mice, while having little evident toxicity to mammalian cells.^[2]

References

^ US 2015175613, Biggart A, et al., "Compounds and compositions for the treatment of parasitic diseases", published 25 June 2015, assigned to Novartis AG
^ Khare S, Nagle AS, Biggart A, Lai YH, Liang F, Davis LC, et al. (September 2016). "Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness". Nature. 537 (7619): 229–233. Bibcode:2016Natur.537..229K. doi:10.1038/nature19339. PMC 5161665. PMID 27501246.

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[1] US 2015175613, Biggart A, et al., "Compounds and compositions for the treatment of parasitic diseases", published 25 June 2015, assigned to Novartis AG

[pmid27501246-2] Khare S, Nagle AS, Biggart A, Lai YH, Liang F, Davis LC, et al. (September 2016). "Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness". Nature. 537 (7619): 229–233. Bibcode:2016Natur.537..229K. doi:10.1038/nature19339. PMC 5161665. PMID 27501246.

[1]

[2]

See also

References