Compounds > l 697639
Page last updated: 2024-11-06

l 697639

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

Description

L 697639: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60832
CHEMBL ID37803
SCHEMBL ID6367001
MeSH IDM0191634

Synonyms (25)

Synonym
3benzoxazolmenh deriv.
3-[[(4,7-dimethylbenzoxazol-2-yl)-methyl]amino]-5-ethyl-6-methylpyridin-2(1h)-one
bdbm1314
3-{[(4,7-dimethyl-1,3-benzoxazol-2-yl)methyl]amino}-5-ethyl-6-methyl-1,2-dihydropyridin-2-one
3-[(4,7-dimethyl-2-benzoxazolylmethyl)amino]-5-ethyl-6-methylpyridin-2(1h)-one
l-697,639
135525-77-8
3-[(4,7-dimethyl-1,3-benzoxazol-2-yl)methylamino]-5-ethyl-6-methyl-1h-pyridin-2-one
l 697639
CHEMBL37803
hnd0yp0tjg ,
2(1h)-pyridinone, 3-(((4,7-dimethyl-2-benzoxazolyl)methyl)amino)-5-ethyl-6-methyl-
3-(((4,7-dimethyl-1,3-benzoxazol-2-yl)methyl)amino)-5-ethyl-6-methylpyridin-2(1h)-one
unii-hnd0yp0tjg
drg-0101
SCHEMBL6367001
VDZJXIOFISBBLT-UHFFFAOYSA-N
3-[(4,7-dimethylbenzoxazol-2-yl)methylamino]-5-ethyl-6-methyl-2(1h)-pyridinone
3-[((4,7-dimethylbenzoxazol-2-yl)methyl)amino]-5-ethyl-6-methyl-2-(1h)-pyridinone
3-[(4,7-dimethylbenzoxazol2-yl)methylamino]-5-ethyl-6-methyl-2(1h)pyridinone
DTXSID50159456
l-697639
3-(((4,7-dimethyl-2-benzoxazolyl)methyl)amino)-5-ethyl-6-methyl-2(1h)-pyridinone
3-(((4,7-dimethylbenzo[d]oxazol-2-yl)methyl)amino)-5-ethyl-6-methylpyridin-2(1h)-one
AKOS040748699

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Single doses of 200 mg and 500 mg resulted in an increase in AUC and Cmax that was less than proportional to the increase in dose."( Human pharmacokinetics and tolerability of L-697,639, a non-nucleoside HIV-1 reverse transcriptase inhibitor.
Au, T; De Lepeleire, I; De Schepper, PJ; Depre, M; Laskin, O; Van Hecken, A; Woolf, E; Yeh, KC, 1994)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)0.02000.00060.91418.3200AID1795306; AID1795378
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.02000.00011.076810.0000AID197804; AID198241
[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 (8)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
AID79111Compound was 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (100.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.05

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

MetricThis Compound (vs All)
Research Demand Index12.05 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
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.		3.0750cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
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.		4.87811,3-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.		1.9810azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
l 693593
L 693593: structure given in first source		2.3820
l-697661
L-697661: HIV-1 reverse transcriptase inhibitor		2.8940
l 696040
L 696040: structure given in first source		2.6730
thiouracil
Thiouracil: Occurs in seeds of Brassica and Crucifera species. Thiouracil has been used as antithyroid, coronary vasodilator, and in congestive heart failure although its use has been largely supplanted by other drugs. It is known to cause blood dyscrasias and suspected of terato- and carcinogenesis.. thiouracil : A nucleobase analogue that is uracil in which the oxo group at C-2 is replaced by a thioxo group.		1.9810nucleobase analogue;
thiocarbonyl compound		antithyroid drug;
metabolite
r 82150
R 82150: structure given in first source; inhibits HIV-1 replication		2.6730
r-82913
R-82913: antiviral target on reverse transcriptase of HIV-1		2.3820
oligonucleotides
[no description available]		1.9710
ConditionIndicatedRelationship StrengthStudiesTrials
AIDS Seroconversion
[description not available]		01.9810