Compounds > wr 243251
Page last updated: 2024-11-08

wr 243251

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

Description

WR 243251: WR 250547 is the (R)-isomer of WR 243251; WR 250548 is the (S)-isomer of WR 243251 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID547231
CHEMBL ID116408
SCHEMBL ID10970969
SCHEMBL ID10971849
MeSH IDM0197914

Synonyms (22)

Synonym
3-dcdad
80092-76-8
wr 250548
(3-(n,n-dimethylamino)propyl)imino-7-chloro-3-(2,4-dichlorophenyl)-3,4-dihydro-1,9(2h,10h)-acridinedione
wr 250547
9(2h)-acridinone, 7-chloro-3-(2,4-dichlorophenyl)-1-((3-(dimethylamino)propyl)amino)-1,3,4,10-tetrahydro-
7-chloro-3-(2',4'-dichlorophenyl)-1-((3'-(dimethylamino)propyl)imino)-1,2,3,4-tetrahydro-9(10h)-acridinone
wr 243251
wr-243251
CHEMBL116408
(r)-7-chloro-3-[2,4-dichlorophenyl]-1,2,3,4-tetrahydro-1-[[3-[dimethylamino]propyl]imino]-9-acridinol
(1e)-7-chloro-3-(2,4-dichlorophenyl)-1-([(e)-3-(dimethylamino)propyl]imino)-1,2,3,4-tetrahydro-9-acridinol #
QPVVEWNCFBEZTH-SGWCAAJKSA-N
QPVVEWNCFBEZTH-UHFFFAOYSA-N
7-chloro-3-(2,4-dichlorophenyl)-1-[[3-(dimethylamino)propyl]imino]-1,3,4,10-tetrahydro-9(2h)acridinone
SCHEMBL10970969
SCHEMBL10971849
7-chloro-3-(2,4-dichlorophenyl)-1-[3-(dimethylamino)propylimino]-2,3,4,10-tetrahydroacridin-9-one
wr243251
DTXSID901000959
7-chloro-3-(2,4-dichlorophenyl)-1-{[3-(dimethylamino)propyl]amino}-3,4-dihydroacridin-9(2h)-one
PD159778

Research Excerpts

Overview

WR 243251 is a dihydroacridinedione that was evaluated for antimalarial blood schizonticidal activity in vitro and in vivo.

ExcerptReferenceRelevance
"WR 243251 is a dihydroacridinedione that was evaluated for antimalarial blood schizonticidal activity in vitro and in vivo. "( Antimalarial activity of WR 243251, a Dihydroacridinedione.
Ager, A; Andersen, SL; Berman, J; Brown, L; Ellis, W; McGreevy, P; Miller, R; Rossan, R; Schuster, BG, 1994)		2.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID135284Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 40 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID606578Cytotoxicity index, ratio of EC50 for mouse J774 cells to EC50 for chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID135282Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 20 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID606570Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID606571Antimalarial activity against chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID140699Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 5 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135283Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after subcutaneous 320 mg/kg dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135286Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after subcutaneous 640 mg/kg dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135280Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 10 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135285Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 5 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135287Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 80 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID135281Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after subcutaneous 160 mg/kg dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
AID606572Resistance index, ratio of EC50 for chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B to EC50 for chloroquine and pyrimethamine-resistant Plasmodium falciparum W22011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships.
AID140694Antimalarial activity in Plasmodium berghei infected mice (Mus musculus) after 10 mg/kg subcutaneous dose1992Journal of medicinal chemistry, Sep-18, Volume: 35, Issue:19
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (50.00)18.2507
2000's2 (33.33)29.6817
2010's1 (16.67)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: 12.36

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 Index12.36 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.36)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.0610aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		2.8910aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
acridines
Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.		450acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene		genotoxin
menoctone
[no description available]		2.8910
halofantrine
halofantrine: used in treatment of mild to moderate acute malaria		2.8910phenanthrenes
salicylhydroxamic acid
[no description available]		210hydroxamic acid;
phenols		antibacterial drug;
EC 1.11.2.2 (myeloperoxidase) inhibitor;
EC 3.5.1.5 (urease) inhibitor;
trypanocidal drug
floxacrine
[no description available]		3.630
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		2.4320hydroxy-1,2-naphthoquinone
1,3,4,10-Tetrahydro-9(2H)-acridinone
[no description available]		2.0610acridines
tafenoquine
tafenoquine : A racemate comprising equimolar amounts of (R)- and (S)-tafenoquine.. N(4)-{2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl}pentane-1,4-diamine : An aminoquinoline that is 8-aminoquinoline which is substituted by methoxy groups at positions 2 and 6, a methyl group at position 4, and a m-(trifluoromethyl)phenoxy group at position 5, and in which the amino substituent at position 8 is itself substituted by a 5-aminopentan-2-yl group.		2.8910(trifluoromethyl)benzenes;
aminoquinoline;
aromatic ether;
primary amino compound;
secondary amino compound
wr 242511
WR 242511: RN given refers to parent cpd		2.8910
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		3.3120
artenimol
artenimol: derivative of antimalarial drug artemisinin (quinghaosu)		2.0610
phenanthrenes
Phenanthrenes: POLYCYCLIC AROMATIC HYDROCARBONS composed of three fused BENZENE rings.. phenanthrenes : Any benzenoid aromatic compound that consists of a phenanthrene skeleton and its substituted derivatives thereof.		2.8910
ConditionIndicatedRelationship StrengthStudiesTrials
Infections, Plasmodium
[description not available]		01.9810
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.		01.9810
Plasmodium falciparum Malaria
[description not available]		02.420
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.420