Page last updated: 2024-11-13

scyx 7158

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID44178354
CHEMBL ID2347704
CHEBI ID183111
SCHEMBL ID1164186
MeSH IDM0556870

Synonyms (31)

Synonym
CHEBI:183111
1266084-51-8
acoziborole
4-luoro-n-(1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-2-(triluoromethyl)benzamide
unii-2ior2oo3gw
4-fluoro-n-(1-hydroxy-3,3-dimethyl-1,3-dihydro-benzo(c)(1),(2)oxaborol-6-yl-2-trifluoromethyl benzamide
2ior2oo3gw ,
benzamide, n-(1,3-dihydro-1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-4-fluoro-2-(trifluoromethyl)-
acoziborole [who-dd]
acoziborole [inn]
scyx-7158
CHEMBL2347704
sctx-7158
4-fluoro-n-(1-hydroxy-3,3-dimethyl-1,3-dihydro-benzo[c][1,2]oxaborol-6-yl)-2-trifluoromethyl benzamide
SCHEMBL1164186
4-fluoro-n-(1-hydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)-2-(trifluoromethyl)benzamide
A937430
DB13086
CS-0016944
HY-19910
n-(1,3-dihydro-1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-4-fluoro-2-(trifluoromethyl)benzamide
mfcd30532746
4-fluoro-n-(1-hydroxy-3,3-dimethyl-1,3-dihydro-2,1-benzoxaborol-6-yl)-2-(trifluoromethyl)benzamide
AS-55745
an5568
W19688
Q27254793
4-fluoro-n-(1-hydroxy-3,3-dimethyl-2,1-benzoxaborol-6-yl)-2-(trifluoromethyl)benzamide
AKOS037644970
DTXSID301336035
AC-36374

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Our compound optimization that has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly potent, orally bioavailable inhibitor of trypanosome replication."( Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
Behera, R; Edwards, P; Guyett, PJ; Karver, CE; Mensa-Wilmot, K; Patel, G; Pollastri, MP; Roncal, NE; Sullenberger, C, 2013
)
0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
(trifluoromethyl)benzenesAn organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1368578Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as infection cure rate at 25 mg/kg, po qd for 7 days starting 21 days post-infection (Rvb = 0%)2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1774613Antileishmanial activity against promastigote form of Leishmania donovani overexpressing Asn232His-mutant of CPSF32021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1435177Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 50 to 51 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1774614Antileishmanial activity against promastigote form of Leishmania donovani overexpressing wild-type CPSF32021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1435176Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 43 to 45 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID739090Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lister 427 after 48 hrs by hemocytometer2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
AID1850422AUC (0 to 24 hrs) in rat at 25 mg/kg, po2022Bioorganic & medicinal chemistry, 06-01, Volume: 63Boron-Containing heterocycles as promising pharmacological agents.
AID1368443Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream forms2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1435172Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 40 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435171Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 41 to 42 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1454780Antitrypanosomal activity against Trypanosoma brucei brucei after 72 hrs by resazurin-based fluorescence assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
AID1435175Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 39 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435168Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 35 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1575040Trypanocidal activity against Trypanosoma brucei brucei 427 assessed as 50% bacterial killing at 7.2 uM preincubated for 6 hrs followed by compound washout and measured after 48 hrs by hemocytometric method2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.
AID1774520Antileishmanial activity against amastigote stage of Leishmania donovani MHOM/ET/67/L82 infected in mouse peritoneal macrophage assessed as reduction in parasite burden incubated for 5 days by Giemsa staining based microscopic analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1435169Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 36 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435170Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 46 to 49 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435173Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 37 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1774519Antileishmanial activity against amastigote stage of Leishmania infantum MHOM/MA(BE)/67/ITMAP263 infected in mouse peritoneal macrophage assessed as reduction in parasite burden incubated for 5 days by Giemsa staining based microscopic analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1368588Time duration during which drug level in brain stays at or above MIC for antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Webster mouse at 25 mg/kg, po bid2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1575028Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by PrestoBlue dye based fluorescence assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.
AID1774612Antileishmanial activity against promastigote form of wild-type Leishmania donovani2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1435174Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 38 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435178Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 52 to 180 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1850421Cmax in rat at 25 mg/kg, po2022Bioorganic & medicinal chemistry, 06-01, Volume: 63Boron-Containing heterocycles as promising pharmacological agents.
AID1435167Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 34 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1774518Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
AID1774615Antitrypanosomal activity against bloodstream form of trypanosoma brucei brucei 427 assessed as reduction in parasitic growth after 72 hrs by resazurin staining based fluorescence assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (71.43)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.74 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (28.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (71.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]