GNF6702
{{Short description|Chemical compound}}
{{Drugbox
| 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
| image = GNF6702_structure.png
| tradename =
| legal_US =
| legal_status =
| bioavailability =
| metabolism =
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| CAS_number_Ref = {{cascite|correct|CAS}}
| CAS_number = 1799329-72-8
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 9NKU4X5ZKZ
| PubChem = 91810392
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 133824
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| ChemSpiderID = 58827646
| C=22 | H=16 | F=1 | N=7 | O=3
| smiles = n5ccccc5-c(cn1n4)cnc1nc4-c3cc(ccc3F)NC(=O)c2oc(C)nc2C
| StdInChI = 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)
| StdInChIKey = 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,{{cite patent | title = Compounds and compositions for the treatment of parasitic diseases | country = US | number = 2015175613 | inventor = Biggart A, et al. | assign1 = Novartis AG | pubdate = 25 June 2015 }} 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.{{cite journal | vauthors = Khare S, Nagle AS, Biggart A, Lai YH, Liang F, Davis LC, Barnes SW, Mathison CJ, Myburgh E, Gao MY, Gillespie JR, Liu X, Tan JL, Stinson M, Rivera IC, Ballard J, Yeh V, Groessl T, Federe G, Koh HX, Venable JD, Bursulaya B, Shapiro M, Mishra PK, Spraggon G, Brock A, Mottram JC, Buckner FS, Rao SP, Wen BG, Walker JR, Tuntland T, Molteni V, Glynne RJ, Supek F | display-authors = 6 | title = Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness | journal = Nature | volume = 537 | issue = 7619 | pages = 229–233 | date = September 2016 | pmid = 27501246 | pmc = 5161665 | doi = 10.1038/nature19339 | bibcode = 2016Natur.537..229K }}
See also
References
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{{Excavata antiparasitics}}
{{Antimicrobial-stub}}