Page last updated: 2024-11-06

kynostatin 227

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

Description

kynostatin 227: structure given in first source; contains allophenylnorstatine as a transition-state mimic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65012
CHEMBL ID231622
SCHEMBL ID2772022
MeSH IDM0208801

Synonyms (15)

Synonym
(4r)-n-tert-butyl-3-[(2s,3s)-2-hydroxy-3-[(2r)-2-[2-(isoquinolin-5-yloxy)acetamido]-3-(methylsulfanyl)propanamido]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
bdbm719
chembl231622 ,
kynostatin 227
kni-227
kynostatin-227
n-(1,1-dimethylethyl)-3-[2-hydroxy-3-[[2-[[(5-isoquinolinyloxy)acetyl]amino]-3-methylthio)-1-oxopropyl]amino]-1-oxo-4-phenylbutyl]-5,5-dimethyl]-4-thiazolidinecarboxamide,[4r-[3[2s*,3s*(r*)],4r*]]
qoa-mta-apns-thz-nh-tbu
(4r)-n-tert-butyl-3-[(2s,3s)-2-hydroxy-3-[[(2r)-2-[[2-(5-isoquinolyloxy)acetyl]amino]-3-methylsulfanyl-propanoyl]amino]-4-phenyl-butanoyl]-5,5-dimethyl-thiazolidine-4-carboxamide
147384-69-8
(4r)-n-tert-butyl-3-[(2s,3s)-2-hydroxy-3-[[(2r)-2-[(2-isoquinolin-5-yloxyacetyl)amino]-3-methylsulfanylpropanoyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide
4-thiazolidinecarboxamide, n-(1,1-dimethylethyl)-3-(2-hydroxy-3-((2-(((5-isoquinolinyloxy)acetyl)amino)-3-(methylthio)-1-oxopropyl)amino)-1-oxo-4-phenylbutyl)-5,5-dimethyl-, (4r-(3(2s*,3s*(r*)),4r*))-
4-thiazolidinecarboxamide, n-(1,1-dimethylethyl)-3-((2s,3s)-2-hydroxy-3-(((2r)-2-(((5-isoquinolinyloxy)acetyl)amino)-3-(methylthio)-1-oxopropyl)amino)-1-oxo-4-phenylbutyl)-5,5-dimethyl-, (4r)-
SCHEMBL2772022
DTXSID30163692

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" In this study, we developed an HPLC assay system for KNI-227 and KNI-272 in rat plasma and examined the pharmacokinetic characteristics in rats after both intravenous (i."( Comparison of a new orally potent tripeptide HIV-1 protease inhibitor (anti-AIDS drug) based on pharmacokinetic characteristics in rats after intravenous and intraduodenal administrations.
Kiriyama, A; Kisanuki, S; Kiso, Y; Mimoto, T; Takada, K, 1993
)
0.29

Bioavailability

ExcerptReferenceRelevance
" The present study demonstrated that JE-2147 has potent antiviral activities in vitro and exhibits good oral bioavailability and plasma pharmacokinetic profiles in two species of laboratory animals."( Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
Fukazawa, T; Hayashi, H; Kato, R; Kiso, Y; Mimoto, T; Misawa, S; Nojima, S; Sato, H; Shintani, M; Takaku, H; Terashima, K; Ueno, T, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)Ki0.00000.00000.12203.1000AID1795265; AID1795273
Plasmepsin-2Plasmodium falciparum (malaria parasite P. falciparum)Ki0.03600.00050.17301.0000AID290578
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID290578Inhibition of Plasmodium falciparum plasmepsin-22007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.
AID397609Antiviral activity against HIV22001Journal of natural products, Feb, Volume: 64, Issue:2
Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program.
AID290579Selectivity for Plasmodium falciparum plasmepsin-2 over human cathepsin D2007Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.
AID1795265Protease Inhibition Assay from Article 10.1021/jm980637h: \\Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.\\1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
AID1795273Protease Inhibition Assay from Article 10.1128/aac.37.4.810: \\In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.\\1993Antimicrobial agents and chemotherapy, Apr, Volume: 37, Issue:4
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.
[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's5 (71.43)18.2507
2000's2 (28.57)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.15

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.15 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]