Compounds > hi 236
Page last updated: 2024-11-10

hi 236

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

Cross-References

ID SourceID
PubMed CID3000498
CHEMBL ID240416
SCHEMBL ID6246077
MeSH IDM0305494

Synonyms (16)

Synonym
1-(5-bromo-2-pyridyl)-3-[2-(2,5-dimethoxyphenyl)ethyl]thiourea
n-[2-(2,5-dimethoxyphenethyl)]-n'-[2-(5-bromopyridyl)]-thiourea
hi-236
d-pbt
dde236
CHEMBL240416 ,
1-(5-bromopyridin-2-yl)-3-[2-(2,5-dimethoxyphenyl)ethyl]thiourea
1-(5-bromopyridin-2-yl)-3-(2,5-dimethoxyphenethyl)thiourea
1-(2,5-dimethoxyphenethyl)-3-(5-bromopyridin-2-yl)thiourea
1-(5-bromo-pyridin-2-yl)-3-[2-(2,5-dimethoxy-phenyl)-ethyl]-thiourea
bdbm50206060
SCHEMBL6246077
233271-65-3
n-(5-bromopyridin-2-yl)-n'-[2-(2,5-dimethoxyphenyl)ethyl]carbamimidothioic acid
n-[2-(2,5-dimethoxyphenylethyl)]-n'-[2-(5-bromopyridyl)]-thiourea
AKOS040746897
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.06650.00011.076810.0000AID197785; AID198231; AID411652; AID491848
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (22)

Assay IDTitleYearJournalArticle
AID491847Cytotoxicity against human MT2 cells after 5 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.
AID491770Antiviral activity against HIV1 3B infected in human MT-2 cells assessed as inhibition of viral-mediated cell death after 5 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.
AID306639Therapeutic index, ratio of IC50 for human MT2 cells to EC50 for HIV1 3B2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor.
AID152657Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17 variant.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID144632The compound was evaluated for percent reduction of H2O2-induced H2DCFDA fluorescence in NALM-6-B-cells.2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.
AID152775Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain RT-MDR.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID411655Therapeutic index, ratio of CC50 for HIV1 Y181C mutant infected human MT2 cells to EC50 for HIV1 with reverse transcriptase Y181C mutation2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID411650Cytotoxicity against mock-infected human MT2 cells after 5 days by MTT assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID152661Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain HTLV IIIB wild type.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID306637Antiviral activity against HIV1 3B in MT2 cells assessed as inhibition of viral-mediated T-cell death by MTT method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor.
AID228862Antioxidant activity was evaluated by measuring the inhibition of oxidation of ABTS to ABTS+ by metmyoglobin in the presence of H2O2.2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.
AID411652Inhibition of HIV1 3B reverse transcriptase2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID411654Cytotoxicity against HIV1 Y181C mutant infected human MT2 cells after 5 days by MTT assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID491848Inhibition of HIV1 reverse transcriptase-mediated thymidine incorporation into D23/D36 primer-template preincubated for 15 mins by polyacrylamide gel-electrophoresis2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
[d4U]-spacer-[HI-236] double-drug inhibitors of HIV-1 reverse-transcriptase.
AID45820The compound was evaluated for percent reduction of H2O2-induced H2DCFDA fluorescence in human CEM T-cells. 2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.
AID411653Antiviral activity against nevirapine-resistant HIV1 with reverse transcriptase Y181C mutation in human MT2 cells assessed as inhibition of viral replication after 5 days by MTT assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID152659Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID306638Cytotoxicity against human MT2 cells2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
[d4U]-butyne-[HI-236] as a non-cleavable, bifunctional NRTI/NNRTI HIV-1 reverse-transcriptase inhibitor.
AID411651Therapeutic index, ratio of CC50 for human MT2 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors.
AID197785Inhibition of recombinant HIV-1 reverse transcriptase2000Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.
AID198231Inhibition of purified recombinant HIV-1 reverse transcriptase1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID411649Antiviral activity against nevirapine-resistant HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication after 5 days by MTT assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
C-2-aryl O-substituted HI-236 derivatives as 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 (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (20.00)18.2507
2000's3 (60.00)29.6817
2010's1 (20.00)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: 30.58

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 Index30.58 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index29.80 (26.88)
Search Engine Supply Index1.80 (0.95)

This Compound (30.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)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.		210cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
propyl gallate
Propyl Gallate: Antioxidant for foods, fats, oils, ethers, emulsions, waxes, and transformer oils.		210trihydroxybenzoic acid
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.		210aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		210alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.4520dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
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.		2.420azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
emivirine
emivirine: a non-nucleoside inhibitor of HIV-1 reverse transcriptase. emivirine : A pyrimidone that is uracil which is substituted at positions 1, 5 and 6 by ethoxymethyl, isopropyl, and benzyl groups, respectively. A non-nucleoside inhibitor of HIV-1 reverse transcriptase, emivirine was an unsuccessful experimental agent for the treatment of HIV.		210pyrimidoneantiviral drug;
HIV-1 reverse transcriptase inhibitor
trovirdine
trovirdine: HIV-1 reverse transcriptase inhibitor		210
ConditionIndicatedRelationship StrengthStudiesTrials