Page last updated: 2024-11-13

nitd008

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Description

NITD008: inhibits enterovirus 71 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44633776
CHEMBL ID1630221
SCHEMBL ID1736124
MeSH IDM000599952

Synonyms (24)

Synonym
(2r,3r,4r,5r)-2-(4-amino-pyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-hydroxymethyl-tetrahydrofuran-3,4-diol
(2r,3r,4r,5r)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-(hydroxymethyl)tetrahydrofuran-3,4-diol
nitd008
CHEMBL1630221 ,
NKRAIOQPSBRMOV-NRMKKVEVSA-N
SCHEMBL1736124
7-(2-c-ethynyl-?-d-ribofuranosyl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine
nitd 008
nitd-008
AKOS025396098
1044589-82-3
(2r,3r,4r,5r)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3-ethynyl-5-(hydroxymethyl)oxolane-3,4-diol
7-(2-c-ethynyl-beta-d-ribofuranosyl)-7h-pyrrolo(2,3-d)pyrimidin-4-amine
lki7t3wq2e ,
7h-pyrrolo(2,3-d)pyrimidin-4-amine, 7-(2-c-ethynyl-beta-d-ribofuranosyl)-
unii-lki7t3wq2e
HY-12957
CS-0012827
MS-24137
7h-pyrrolo(2,3-d)pyrimidin-4-amine, 7-(2-c-ethynyl-.beta.-d-ribofuranosyl)-
7-(2-c-ethynyl-.beta.-d-ribofuranosyl)-7h-pyrrolo(2,3-d)pyrimidin-4-amine
bdbm50513993
DTXSID701159354
7-(2-c-ethynyl-beta-d-ribofuranosyl)-7h-pyrrolo[2,3-d]pyrimidin-4-amine

Research Excerpts

Overview

NITD008 is an adenosine analogue inhibitor. It interrupts the RNA-dependent RNA polymerase of flaviviruses.

ExcerptReferenceRelevance
"NITD008 is an adenosine analogue inhibitor that interrupts the RNA-dependent RNA polymerase of flaviviruses."( Combined treatment of adenosine nucleoside inhibitor NITD008 and histone deacetylase inhibitor vorinostat represents an immunotherapy strategy to ameliorate West Nile virus infection.
Nelson, J; Orillo, B; Roe, K; Shi, PY; Verma, S, 2015
)
1.39

Toxicity

ExcerptReferenceRelevance
" Some have hypothesized that the active metabolites of toxic ribonucleoside analogs, the triphosphate forms, inadvertently target human mitochondrial RNA polymerase (POLRMT), thus inhibiting mitochondrial RNA transcription and protein synthesis."( Structure-activity relationship analysis of mitochondrial toxicity caused by antiviral ribonucleoside analogs.
Behera, I; Beigelman, L; Chaudhuri, S; Deval, J; Dyatkina, N; Jekle, A; Jin, Z; Kinkade, A; Rajwanshi, VK; Smith, DB; Symons, JA; Tucker, K; Wang, G, 2017
)
0.46

Dosage Studied

ExcerptRelevanceReference
" However, in vivo pharmacokinetic studies indicated that NITD449 had a low level of exposure in plasma when dosed orally."( Inhibition of dengue virus by an ester prodrug of an adenosine analog.
Chen, YL; Dartois, V; Duraiswamy, J; Goh, A; Keller, TH; Kondreddi, RR; Lakshminarayana, SB; Liu, B; Qing, M; Schul, W; Shi, PY; Weaver, M; Xu, HY; Yin, Z; Yip, A, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NS5 Zika virusEC50 (µMol)0.13700.00870.54751.3000AID1558277; AID1558278; AID1558279; AID1558280
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (103)

Assay IDTitleYearJournalArticle
AID545704Antiviral activity against Dengue virus 2 TSVO1 infected in alpha/beta interferon and INFgamma receptor deficient AG129 mouse assessed as decrease in viral load treated 12 hrs postinfection measured after 3 days of infection by HPLC2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1813110Cytotoxicity against human RD cells assessed as reduction in cell viability by Cell Titer-Glo luminescent cell viability assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1813114Cmax in CD-1 mouse at 25 mg/kg, po by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545702Drug uptake in rat blood assessed as di-derivatives of compound level at 25 mg/kg, po by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1338314Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Identification and biochemical characterization of DC07090 as a novel potent small molecule inhibitor against human enterovirus 71 3C protease by structure-based virtual screening.
AID1860888Selectivity index, ratio of CC50 for human RD cells to IC50 for CA6 infected in human RD cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1813105Half life in CD-1 mouse at 5 mg/kg, iv by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1860870Antiviral activity against ZIKV-SMGC-1 infected in human BHK cells incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545677Cytotoxicity against human A549 cells assessed as intracellular ATP level by Celltiter-Glo luminescent assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1277368Antiviral activity against clinical isolates of Dengue virus 2 Martinique H/IMTSSA-MART/98-703 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID1813113Cmax in CD-1 mouse at 5 mg/kg, iv by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1655476Selectivity index, ratio of CC50 for human HuH7 cells to EC50 for Zika virus H/PF/2013 infected in human HuH7 cells2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
AID545694Selectivity ratio of EC50 for Dengue virus 2 infected in human HEK293 cells in presence of siRNA targeting adenosine kinase to EC50 for Dengue virus 2 infected in human HEK293 cells in absence of siRNA targeting adenosine kinase2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1728710Antiviral activity against dengue virus 2 EDEN 3295 infected in human Huh-7 cells assessed as reduction in virus replication incubated for 48 hrs by plaque reduction assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Sustainable, three-component, one-pot procedure to obtain active anti-flavivirus agents.
AID545705Antiviral activity against Dengue virus 2 TSVO1 infected in alpha/beta interferon and INFgamma receptor deficient AG129 mouse assessed as decrease in viral load at 150 mg/kg, po 12 hrs postinfection measured after 3 days of infection by HPLC2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1558283Cytotoxicity against African green monkey Vero cells2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID545698Drug uptake in rat blood assessed as di-derivatives of compound level at 5 mg/kg, ip by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1813117AUC ( 0 to infinity ) in CD-1 mouse at 5 mg/kg, iv by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1277371Antiviral activity against clinical isolates of Dengue virus 4 Martinique 017 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID545680Cytotoxicity against hamster BHK21 cells assessed as intracellular ATP level upto 100 uM by Celltiter-Glo luminescent assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545687Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 3 uM after 35 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1813106Half life in CD-1 mouse at 25 mg/kg, po by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545690Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral NS3 protein expression at 1 uM after 35 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1655472Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter Glo Luminescent assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
AID1813109Selectivity index, ratio of CC50 for human RD cells to IC50 for Enterovirus A71 infected in human RD cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545693Antiviral activity against Dengue virus 2 infected in human HEK293 cells assessed as level of viral titer after 48 hrs by luciferase reporter gene assay in presence of siRNA targeting adenosine kinase2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545686Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 1 uM after 35 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860877Antiviral activity against EV71 infected in human RD cells incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860880Cytotoxicity against human RD cells infected with EV71 incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860874Antiviral activity against YFV-17D infected in human BHK cells incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1813116AUC ( 0 to last) in CD-1 mouse at 25 mg/kg, po by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1860878Antiviral activity against CA6 infected in human RD cells incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860889Selectivity index, ratio of CC50 for human RD cells to IC50 for CA16 infected in human RD cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860872Cytotoxicity against human BHK cells infected with DENV-NGC-1 incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1813111Antiviral activity against Enterovirus A71 infected in human RD cells assessed as inhibition of viral replication measured after 4 days by Cell Titer-Glo luminescent cell viability assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545689Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral NS3 protein expression at 3 uM after 24 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1813108Antiviral activity against Enterovirus D68 infected in human RD cells assessed as inhibition of viral replication measured after 4 days by Cell Titer-Glo luminescent cell viability assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545700Drug uptake in rat plasma at 25 mg/kg, po by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545682Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 1 uM after 2 to 4 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1277370Antiviral activity against clinical isolates of Dengue virus 4 Dakar HD34460 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID1813115AUC ( 0 to last) in CD-1 mouse at 5 mg/kg, iv by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545703Drug uptake in rat blood assessed as tri-derivatives of compound level at 25 mg/kg, po by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1206538Antiviral activity against dengue virus 2 TSV01 in AG129 mouse model of dengue viremia assessed as log reduction in virus plaques at 25 mg/kg, po BID for 3 days relative to untreated control2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Lead optimization of spiropyrazolopyridones: a new and potent class of dengue virus inhibitors.
AID1558280Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1813118AUC ( 0 to infinity ) in CD-1 mouse at 25 mg/kg, po by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1655473Antiviral activity against Dengue virus 2 EDEN 3295 infected in human HuH7 cells assessed as reduction in virus replication incubated for 48 hrs by plaque reduction assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
AID1860885Selectivity index, ratio of CC50 for human BHK cells to IC50 for JEV-SA14 infected in human BHK cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1338298Antiviral activity against EV71 assessed as reduction in viral replication after 72 hrs by CellTiter-glo luminescent cell viability assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Identification and biochemical characterization of DC07090 as a novel potent small molecule inhibitor against human enterovirus 71 3C protease by structure-based virtual screening.
AID1813104Tmax in CD-1 mouse at 5 mg/kg, iv by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1860884Selectivity index, ratio of CC50 for human BHK cells to IC50 for DENV-NGC infected in human BHK cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860882Cytotoxicity against human RD cells infected with CA16 incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID546797Antiviral activity against Dengue virus 4 MY22713 infected in human A549 cells by CFI assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID1860879Antiviral activity against CA16 infected in human RD cells incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545692Antiviral activity against Dengue virus 2 infected in human A549 cells assessed as level of E protein production up to 20 uM by ELISA in presence of 0.2 uM adenosine kinase inhibitor iodotubercidin2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1558279Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity by measuring viral RNA by RT-qPCR method2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1728709Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescent assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Sustainable, three-component, one-pot procedure to obtain active anti-flavivirus agents.
AID546793Antiviral activity against Dengue virus 2 NGC infected in human A549 cells by CFI assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID1860869Antiviral activity against DENV-NGC-1 infected in human BHK cells incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID546798Antiviral activity against Dengue virus 2 NGC infected in human PBMC cells by plaque assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID1655475Antiviral activity against Zika virus H/PF/2013 infected in human HuH7 cells assessed as reduction in virus replication incubated for 24 hrs by plaque reduction assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
AID545701Drug uptake in rat blood assessed as mono-derivatives of compound level at 25 mg/kg, po by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860875Cytotoxicity against human BHK cells infected with JEV-SA14 incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545676Antiviral activity against at 0.3 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as reduction in viral titer after 48 hrs postinfection2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860881Cytotoxicity against human RD cells infected with CA6 incubated for 3 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545688Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral NS3 protein expression at 1 uM after 24 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1277369Antiviral activity against clinical isolates of Dengue virus 3 Bolivia 4025 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID1813107Selectivity index, ratio of CC50 for human RD cells to IC50 for Enterovirus D68 infected in human RD cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID545679Antiviral activity against at 0.3 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as reduction in viral titer at 6 uM after 48 hrs postinfection2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545706Antiviral activity against Dengue virus 2 TSVO1 infected in alpha/beta interferon and INFgamma receptor deficient AG129 mouse assessed as decrease in viral load at 300 mg/kg, po 12 hrs postinfection measured after 3 days of infection by HPLC2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1728714Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for dengue virus 2 EDEN 3295 infected in human Huh-7 cells2021European journal of medicinal chemistry, Jan-15, Volume: 210Sustainable, three-component, one-pot procedure to obtain active anti-flavivirus agents.
AID1277367Antiviral activity against clinical isolates of Dengue virus 1 Indonesia JKT 1186 TVP 949 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID1338313Antiviral activity against EV71 infected in African green monkey Vero cells after 48 hrs by plaque assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Identification and biochemical characterization of DC07090 as a novel potent small molecule inhibitor against human enterovirus 71 3C protease by structure-based virtual screening.
AID1860871Cytotoxicity against human BHK cells infected with ZIKV-SMGC-1 incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545678Antiviral activity against at 0.3 MOI Dengue virus 2 infected in human A549 cells assessed as level of E protein after 48 hrs by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860887Selectivity index, ratio of CC50 for human RD cells to IC50 for EV71 infected in human RD cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID546795Antiviral activity against Dengue virus 2 MY10340 infected in human A549 cells by CFI assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID1277366Antiviral activity against clinical isolates of Dengue virus 2 Trinidad 1751 TC 544 infected in African green monkey Vero E6 cells assessed as reduction in viral RNA after 4 days by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID545685Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 3 uM after 24 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860876Cytotoxicity against human BHK cells infected with YFV-17D incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID545707Antiviral activity against 3x10'7 PFU Dengue virus 2 D2S10 infected in alpha/beta interferon and INFgamma receptor deficient AG129 mouse assessed as protection against lethal virus challenge at 75 mg/kg, po treated 12 hrs postinfection by HPLC2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID547042Antiviral activity against Dengue virus 2 TSV01 infected in AG129 mouse assessed as reduced viremia by 25 mg/kg, po BID for 3 days measured on day 4 by plaque assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID1277365Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability treated for 3 days measured on day 4 by cell titer-blue fluorescent assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Novel 2-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,3,4-oxadiazole and 3-phenyl-5-[(E)-2-(thiophen-2-yl)ethenyl]-1,2,4-oxadiazole derivatives as dengue virus inhibitors targeting NS5 polymerase.
AID545697Drug uptake in rat blood assessed as mono-derivatives of compound level at 5 mg/kg, ip by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1699914Antiviral activity against DENV-2 infected in African green monkey Vero cells assessed as virus titer reduction incubated for 48 hrs by plaque assay2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro.
AID545683Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 3 uM after 2 to 4 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1558278Inhibition of RNA-dependent RNA polymerase in Zika virus FSS13025/2010 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1728715Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for Zika virus H/PF/2013 infected in human Huh-7 cells2021European journal of medicinal chemistry, Jan-15, Volume: 210Sustainable, three-component, one-pot procedure to obtain active anti-flavivirus agents.
AID1655474Selectivity index, ratio of CC50 for human HuH7 cells to EC50 for Dengue virus 2 EDEN 3295 infected in human HuH7 cells2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Pyridobenzothiazolones Exert Potent Anti-Dengue Activity by Hampering Multiple Functions of NS5 Polymerase.
AID545684Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral RNA synthesis at 1 uM after 24 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1860883Selectivity index, ratio of CC50 for human BHK cells to IC50 for ZIKV-SMGC-1 infected in human BHK cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID546796Antiviral activity against Dengue virus 3 MY22366 infected in human A549 cells by CFI assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
AID545699Drug uptake in rat blood assessed as tri-derivatives of compound level at 5 mg/kg, ip by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545691Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as decrease in viral NS3 protein expression at 3 uM after 35 hrs post-transfection by luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545695Antiviral activity against Dengue virus 2 infected in human HEK293 cells assessed as level of viral titer after 48 hrs by luciferase reporter gene assay in presence of siRNA targeting deoxycytidine kinase2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID1728712Antiviral activity against Zika virus H/PF/2013 infected in human Huh-7 cells assessed as reduction in virus replication incubated for 24 hrs by plaque reduction assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Sustainable, three-component, one-pot procedure to obtain active anti-flavivirus agents.
AID1813112Tmax in CD-1 mouse at 25 mg/kg, po by LC-MS/MS2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and evaluation of 2'-acetylene-7-deaza-adenosine phosphoamidate derivatives as anti-EV71 and anti-EV-D68 agents.
AID1558277Inhibition of RNA-dependent RNA polymerase in Zika virus GZ01/2016 infected in African green monkey Vero cells assessed as antiviral activity measured 48 hrs post infection by plaque assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID1860873Antiviral activity against JEV-SA14 infected in human BHK cells incubated for 7 days by CellTiter 96 luminescent cell viability assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1860886Selectivity index, ratio of CC50 for human BHK cells to IC50 for YFV-17D infected in human BHK cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro.
AID1700577Antiviral activity against Zika virus Z16019 infected in human A549 cells assessed as reduction in viral titer preincubated for 1 hr followed by compound washout and subsequent compound addition without virus and measured after 48 hrs by plaque assay
AID545681Antiviral activity against at 1 MOI of Dengue virus 2 infected in hamster BHK21 cells assessed as viral titer after 48 hrs postinfection by plaque assay2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID545696Drug uptake in rat plasma at 5 mg/kg, ip by fast protein liquid chromatography2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Inhibition of dengue virus RNA synthesis by an adenosine nucleoside.
AID546794Antiviral activity against Dengue virus 1 MY10245 infected in human A549 cells by CFI assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Inhibition of dengue virus by an ester prodrug of an adenosine analog.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's17 (70.83)24.3611
2020's7 (29.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.06

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 Index24.06 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index5.64 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other23 (95.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]