Compounds > l-697661
Page last updated: 2024-11-06

l-697661

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Description

L-697661: HIV-1 reverse transcriptase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65002
CHEMBL ID268871
SCHEMBL ID599639
MeSH IDM0205741

Synonyms (20)

Synonym
bdbm1317
3-[[(4,7-dichlorobenzoxazol-2-yl)-methyl]amino]-5-ethyl-6-methylpyridin-2(1h)-one
3-{[(4,7-dichloro-1,3-benzoxazol-2-yl)methyl]amino}-5-ethyl-6-methyl-1,2-dihydropyridin-2-one
chembl268871 ,
unii-4660n666ez
4660n666ez ,
l-697661
3-[(4,7-dichloro-1,3-benzoxazol-2-yl)methylamino]-5-ethyl-6-methyl-1h-pyridin-2-one
l 697,661
135525-78-9
3-[(4,7-dichlorobenzoxazolylmethyl)amino]-5-ethyl-6-methylpyridin-2(1h)-one
l-697,661
l697,661
3-(((4,7-dichloro-1,3-benzoxazol-2-yl)methyl)amino)-5-ethyl-6-methylpyridin-2(1h)-one
2(1h)-pyridinone, 3-(((4,7-dichloro-2-benzoxazolyl)methyl)amino)-5-ethyl-6-methyl-
SCHEMBL599639
DTXSID10159457
AKOS030539285
bdbm50478741
3-(((4,7-dichlorobenzo[d]oxazol-2-yl)methyl)amino)-5-ethyl-6-methylpyridin-2(1h)-one

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel."( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993)		0.29
" Nevertheless, one compound (13), PNU-103657, possessed oral bioavailability in rats approaching that of the structurally related NNRTI drug delavirdine which is currently on the market for the treatment of HIV infection."( Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
Adams, WJ; Friis, JM; Genin, MJ; Kopta, LA; May, PD; Olmsted, RA; Poel, TJ; Romero, DL; Thomas, RC; Voorman, RL; Yagi, Y, 1999)		0.3

Dosage Studied

ExcerptRelevanceReference
" Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel."( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)6.99860.00060.91418.3200AID1795306; AID1795311; AID1795346; AID1795349; AID1795367; AID1795378; AID1795381; AID1795382
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)3.22090.00011.076810.0000AID143393; AID197779; AID197787; AID197788; AID197792; AID197795; AID197803; AID197804; AID197807; AID197941; AID197943; AID197944; AID197948; AID198069; AID198241; AID198396; AID198397; AID198409; AID198410; AID198411; AID199242; AID199243; AID360699; AID360700; AID360701; AID360702; AID360703; AID360704; AID360705; AID360706; AID360707; AID360708; AID360709; AID360710; AID360711; AID360712; AID360713; AID360714; AID360715; AID360716; AID360718; AID360719
Protease Human immunodeficiency virus 1IC50 (µMol)8.52700.00010.22487.3200AID200169; AID200170; AID200171
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC50 (µMol)0.00700.00040.61539.7000AID200005
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED500.06500.00020.99359.8000AID105522
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC95 (µMol)0.10000.10000.45000.8000AID106773
Protease Human immunodeficiency virus 1IC90 (µMol)0.80000.00200.67847.3000AID143398
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (2)

Processvia Protein(s)Taxonomy
viral life cycleGag-Pol polyproteinHIV-1 M:B_HXB2R
establishment of integrated proviral latencyGag-Pol polyproteinHIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
peptidase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
integrase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (114)

Assay IDTitleYearJournalArticle
AID81442Inhibition of HIV-1 D34 replication in human peripheral blood mononuclear cells.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID198069Inhibition of reverse transcriptase activity of HIV-1 in the presence of [alpha35 S] TTP as cosubstrate.1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID360725Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 6 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID197779Ability to inhibit HIV-1 Reverse Transcriptase (RT) using an rC-dG template/primer1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID360721Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto one deoxyribonucleotide2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID83090In vitro antiviral activity against NNRTI-resistant DLVR-IIIB (L100I) HIV-1 variant1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
AID105716Antiviral activity against HIV-1 (strain RF) infected MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID105715Antiviral activity against HIV-1 resistant to 2-(2-Benzoyl-4-chloro-phenyl)-N-[4-(3-dimethylamino-propoxy)-2-methyl-phenyl]-acetamide in MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID360723Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 2 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID106778Compound was evaluated for antiviral activity in MT-4 cells. Cell culture inhibitor concentration (CIC95) is defined as concentration which inhibited >95% the spread of HIV-1 IIIb infection in susceptible cell culture; value ranges from 0.025-0.050 uM1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
AID360705Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID143398Compound was evaluated for its ability to inhibit the mutant K103N NNRTI HIV-1 enzyme2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID199243Inhibitory effect on recombinant HIV- 1 reverse transcriptase which has a mutation Tyr 181 to Cys 181 (clone 90)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID199242Inhibitory effect on recombinant HIV- 1 reverse transcriptase which has a mutation Leu 100 to Ile 100 (clone 118)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID104944Concentration which reduced the viability of the HIV-1 infected MT-4 cells to 50% compared to untreated control cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID153130Effective dose for inhibition of viral replication in cell culture of 0.1 uM2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID200171Inhibition single mutant of HIV-1 RT (Y181C)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID143395Antiviral activity against HIV-1 in MT-2 (human leukemia) cells in vitro.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID360702Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using RNA PPT primed-DNA hybrid substrate2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID105547Tested for the inhibition of wild type HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID360717Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 6 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360724Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 3 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID81443Inhibition of HIV-1 IIIB replication in MT2 (human lymphocyte) cells.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID105545Inhibition of mutant type (Cys181) HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID360720Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360726Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 9 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID92062Percent unbound determined for whole normal human plasma1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
AID44828Inhibition of p24 antigen formation in infected C8166-cells1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID104244Cytotoxic concentration against MT-2 cells1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID198409Tested for the inhibition of mutant type (Cys181) HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID197795Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID197944In vitro inhibition of recombinant reverse transcriptase (WT) of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID198397Tested for inhibition against HIV-1 RT (used (poly)rC-(oligo)dG as the template)1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
AID360708Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360706Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360722Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID83093In vitro antiviral activity against NNRTI-resistant IIIB (WT) HIV-1 variant1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
AID83092In vitro antiviral activity against NNRTI-resistant DLVR-MF (P236L) HIV-1 variant1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
AID104954Concentration which inhibited >95% spread of HIV-1 strain IIIb infection in susceptible MT-4 cell culture1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
AID197804In vitro HIV-1 RT inhibitory activity using rC.dG as template-primer1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
AID105522Concentration which reduced the cytopathic effect of HIV-1 in MT-4 infected cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID153102Cytotoxic concentration against PBMC cells1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID143403Compound was evaluated for its ability to inhibit the mutant K103N V1081NNRTI HIV-1 enzyme; ND= not determined2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID197948In vitro inhibitory concentration against HIV-1 reverse transcriptase using rC-dG template primer1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
AID198410Tested for the inhibition of mutant type (Ile100) HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID200169Inhibition of HIV-1 RT using rC-dG as template1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID83096In vitro antiviral activity against NNRTI-resistant R88703R-IIIB (Y181C) HIV-1 variant1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
AID81772Concentration required to inhibit P24 production by 90% against U-90,152 of HIV-1 MF (P236L)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID360727Inhibition of HIV1 RT D443N mutant mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 12 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID200170Inhibition single mutant of HIV-1 RT (K103 N)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID143393Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay.2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID360718Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 9 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID197941In vitro inhibition of mutant P236L recombinant reverse transcriptase of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID79232Concentration which inhibited >95% spread of HIV-1 strain IIIb infection in susceptible H-9 cell culture1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
AID360714Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto one deoxyribonucleotide2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID198396Inhibitory activity against HIV-1 reverse transcriptase (HIV-RT)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID360713Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID153129Cytotoxic concentration was determined2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID360704Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID81770Concentration required to inhibit P24 production by 90% against U-90,152 of HIV-1 IIIB (L100I, M230L)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID198593In vitro inhibition of HIV-1 reverse transcriptase at 100 uM1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID197807In vitro inhibition of HIV-1 reverse transcriptase1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID105571Antiviral activity was determined against wild type HIV-1 in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID143401Compound was evaluated for its ability to inhibit the mutant K103N P225H NNRTI HIV-1 enzyme; ND= not determined2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID360700Inhibition of HIV1 RT mediated DNA-dependent plus-strand DNA polymerization after 5 mins by gel-based assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID105891Cytotoxicity against uninfected MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID360710Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID105000Inhibitory concentration which prevents the spread of HIV-1 IIIB infection in MT2 T-lymphoid cells1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID360701Inhibition of HIV1 RT mediated DNA-dependent plus strand synthesis initiation using RNA-DNA hybrid substrate2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360703Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using DNA PPT-primed substrate2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID197788In vitro ability to inhibit wild type resistant (WT) reverse transcriptase2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID83095In vitro antiviral activity against NNRTI-resistant L-697661R-IIIB (Y181C) HIV-1 variant1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
AID44829Inhibition of syncytia formation in infected C8166-cells1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID197787In vitro ability to inhibit mutant P236L reverse transcriptase2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID197792Compound was tested for Inhibition of HIV-1 RT activity.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.
AID79109Compound is evaluated for antiviral activity in H9 cells. Cell culture inhibitor concentration (CIC95) is defined as uM1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
AID106775Inhibition of cell culture in MT-4 cells1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID104963Compound was evaluated for the anti-viral activity against cultured MT-4 cells1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID81768Concentration required to inhibit P24 production by 90% against L-697661 of HIV-1 IIIB (Y181C)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID360709Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360716Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 3 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360715Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 2 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID197943In vitro inhibition of mutant Y181C recombinant reverse transcriptase of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID143397Compound was evaluated for its ability to inhibit the mutant K103N L1001 NNRTI HIV-1 enzyme; ND= not determined2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
AID27059Half life was determined1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
AID360728Displacement of [3H]ATP binding to HIV1 RT associated with RNA PPT-primed DNA template substrate2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID105566Antiviral activity was determined against HIV-1 (clone 118) in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID81422Antiviral activity against BHAP-resistant viral strain HIV-1 MF using Delaviridine (U-90512) as a comparator.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
AID198411Tested for the inhibition of wild type HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID200005Inhibition of reverse transcriptase of HIV-1 (strain RF)-infected MT-4 cells in RPMI 1640 growth medium in MTM assay1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID360712Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID104281Inhibition of HIV-1 (strain A17)-infected MT-4 cells1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID106774Cell culture inhibitory concentration against spread of HIV-I infection in MT-4 cells was determined1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
AID197803Inhibitory effect on wild type HIV- 1 reverse transcriptase using rCdG as template and dGTP as substrate.1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID81421Antiviral activity against BHAP-resistant viral strain HIV-1 IIIB using Delaviridine (U-90512) as a comparator.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
AID105573Antiviral activity was determined against wild type HIV-1 in MT-4 cells infected with HIV-1 IIIB using an XTT assay using 15% human AB serum; NT means not tested1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID81423Antiviral activity against L-drug-resistant viral strain HIV-1 IIIB using L-697,661 as a comparator.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
AID198241Inhibitory activity against HIV-1 reverse transcriptase (RT)1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
AID360699Inhibition of HIV1 RT mediated RNA-dependent minus-strand DNA synthesis after 5 mins by gel-based assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID105568Antiviral activity was determined against HIV-1 (clone 90) in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID360711Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID106773Cell culture inhibitor concentration required to inhibit the spread of HIV-1 strain III B infection in MT-4 human T-lymphoid cells1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
AID105546Inhibition of mutant type (Ile100) HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID360719Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization using chimeric substrate with RNA PPT primer extended at 3' end with upto 12 deoxyribonucleotides2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID360707Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID1795306HIV-1 RT Assay from Article 10.1021/jm00099a007: \\Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.\\1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
AID1795367HIV-1 RT Assay from Article 10.1021/jm950639r: \\Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.\\1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1795381HIV-1 RT Assay from Article 10.1021/jm00061a022: \\5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.\\1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID1795349HIV-1 RT Assay from Article 10.1021/jm960158n: \\Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.\\1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID1795311HIV-1 RT Assay from Article 10.1021/jm00069a011: \\Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.\\1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID1795346HIV-1 RT Assay from Article 10.1021/jm00025a010: \\Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.\\1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID1795382HIV-1 RT Assay from Article 10.1021/jm00062a027: \\Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-c1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID1795378HIV-1 RT Assay from Article 10.1021/jm00113a036: \\2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.\\1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
AID493017Wombat Data for BeliefDocking1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's37 (92.50)18.2507
2000's3 (7.50)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: 10.32

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 Index10.32 (24.57)
Research Supply Index3.83 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (12.50%)5.53%
Reviews2 (5.00%)6.00%
Case Studies1 (2.50%)4.05%
Observational0 (0.00%)0.25%
Other32 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pharmacokinetic Study of L-697,661 Alone and in Combination With Zidovudine [NCT00000628]Phase 127 participants InterventionalCompleted
[information is prepared from clinicaltrials.gov, extracted Sep-2024]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		4.2911pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
foscarnet
Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.4120carboxylic acid;
one-carbon compound;
phosphonic acids		antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		11.08230cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
delavirdine
Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		3.4980aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		1.9810amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
leucine
Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.		6.9810amino acid zwitterion;
L-alpha-amino acid;
leucine;
proteinogenic amino acid;
pyruvate family amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		1.9810mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
benzoxazoles
1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.		10.192251,3-benzoxazoles;
mancude organic heterobicyclic parent
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		1.9810
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		8.01125azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
lamivudine
[no description available]		1.9810monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
l 697639
L 697639: structure given in first source		2.8940
atevirdine
atevirdine: inhibits replication of HIV-1; U 87201E is the methanesulfonate salt		3.3770
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.4220acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil
5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil: inhibits human HIV-1; structure given in first source		1.9810
l 693593
L 693593: structure given in first source		2.3820
zidovudine triphosphate
[no description available]		2.0310
u 88204
U 88204: structure given in first source		1.9810
l 696040
L 696040: structure given in first source		2.6730
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		6.9810amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
l 734005
5-chloro-3-phenylthioindole-2-carboxamide: structure given in first source; an inhibitor of HIV-1 reverse transcriptase		1.9810
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		1.9810L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
delavirdine mesylate
delavirdine mesylate : The monomethanesulfonic acid salt of delavirdine, a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		2.420methanesulfonate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor
l 737126
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: structure given in first source; an inhibitor of HIV-1 reverse transcriptase		1.9810
dpc 961
[no description available]		210
r 82150
R 82150: structure given in first source; inhibits HIV-1 replication		3.0850
r-82913
R-82913: antiviral target on reverse transcriptase of HIV-1		4.5880
trovirdine
trovirdine: HIV-1 reverse transcriptase inhibitor		2.6830
ly 73497
LY 73497: HIV-1 reverse transcriptase inhibitor; structure in first source		2.3920
dpc 083
[no description available]		210
2',3'-dideoxyguanosine 5'-triphosphate
[no description available]		1.9810
ConditionIndicatedRelationship StrengthStudiesTrials
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		01.9810
HIV Coinfection
[description not available]		07.9873
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		07.9873
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		01.9810
Viremia
The presence of viruses in the blood.		09.6232
Acquired Immune Deficiency Syndrome
[description not available]		04.0631
Acquired Immunodeficiency Syndrome
An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.		04.0631
AIDS Seroconversion
[description not available]		05.2522
Benign Neoplasms
[description not available]		03.3711
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.3711
Ulcer
A lesion on the surface of the skin or a mucous surface, produced by the sloughing of inflammatory necrotic tissue.		01.9810