bulaquine profile

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

ID Source	ID
PubMed CID	9831444
CHEMBL ID	3770139
CHEBI ID	135558
SCHEMBL ID	5002047
MeSH ID	M0175182

Synonym
bulaquine
CHEBI:135558
tsq6u39q3g ,
bulaquine [inn]
cdri 80-53
cdri 80/53
79781-00-3
compound 80/53
dihydro-3-(1-((4-((6-methoxy-8-quinolyl)amino)pentyl)amino)ethylidene)-2(3h)-furanone
2(3h)-furanone, dihydro-3-(1-((4-((6-methoxy-8-quinolinyl)amino)pentyl)amino)ethylidene)-
n'-(3-acetyl-4,5-dihydro-2-furanyl)-n(4)-(6-methoxy-8-quinolyl)-1,4-pentanediamine
aablaquine
unii-tsq6u39q3g
bulaquine [who-dd]
SCHEMBL5002047
CHEMBL3770139
(3z)-3-[1-[4-[(6-methoxyquinolin-8-yl)amino]pentylamino]ethylidene]oxolan-2-one
3-(1-((4-((6-methoxyquinolin-8-yl)amino)pentyl)amino)ethylidene)dihydrofuran-2(3h)-one
Q27290262
CS-0026779
HY-106866

Excerpt	Reference	Relevance
"Methemoglobin, a toxic ferric form of hemoglobin, is continuously formed in normal erythrocytes, but during abnormal situations in situ, the level is enhanced."	( A simple and rapid evaluation of methemoglobin toxicity of 8-aminoquinolines and related compounds. Jain, GK; Pandey, VC; Puri, SK; Singh, S; Srivastava, P, 2000)	0.31

Excerpt	Reference	Relevance
" The method was applied to determine the pharmacokinetic parameters of AM in 5 rabbits receiving a single bolus intravenous and peroral dose in a crossover study."	( A rapid and sensitive high performance liquid chromatographic assay of the new antimalarial compound 80/53 in serum with a novel sample clean-up method and its pharmacokinetics in rabbits. Gupta, RC; Paliwal, JK, 1998)	0.3

Class	Description
aminoquinoline	Any member of the class of quinolines in which the quinoline skeleton is substituted by one or more amino or substituted-amino groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Assay ID	Title	Year	Journal	Article
AID1282060	Cytotoxicity against HEK293T cells assessed as cell viability after 48 hrs by MTT assay	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8	Novel squaramides with in vitro liver stage antiplasmodial activity.
AID1282058	Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8	Novel squaramides with in vitro liver stage antiplasmodial activity.
AID1282062	Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes after 24 hrs by [3H]-hypoxanthine incorporation assay	2016	Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8	Novel squaramides with in vitro liver stage antiplasmodial activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	3 (14.29)	18.7374
1990's	5 (23.81)	18.2507
2000's	11 (52.38)	29.6817
2010's	2 (9.52)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	4 (18.18%)	5.53%
Reviews	1 (4.55%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	17 (77.27%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
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.	10.43	4	1	aminoquinoline; 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.	8.06	21	4	aminoquinoline; aromatic ether; N-substituted diamine	antimalarial
pyrimethamine Maloprim: contains above 2 cpds	3.27	1	0	aminopyrimidine; monochlorobenzenes	antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sulfadoxine Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.	3.27	1	0	pyrimidines; sulfonamide	antibacterial drug; antimalarial
artemisinin (+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.	2	1	0	organic peroxide; sesquiterpene lactone	antimalarial; plant metabolite
sesquiterpenes [no description available]	2	1	0
quinine [no description available]	5.79	3	2	cinchona alkaloid	antimalarial; muscle relaxant; non-narcotic analgesic
mefloquine Mefloquine: A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.. mefloquine : A racemate composed of (+)-(11R,2'S)- and (-)-(11S,2'R)-enantiomers of mefloquine. An antimalarial agent which acts as a blood schizonticide; its mechanism of action is unknown.	3.27	1	0

Condition	Relationship Strength	Studies	Trials
Infections, Plasmodium [description not available]	2.92	4	0
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.	2.92	4	0
Deficiency of Glucose-6-Phosphate Dehydrogenase [description not available]	3.09	1	0
Plasmodium falciparum Malaria [description not available]	10.6	3	2
Glucosephosphate Dehydrogenase Deficiency A disease-producing enzyme deficiency subject to many variants, some of which cause a deficiency of GLUCOSE-6-PHOSPHATE DEHYDROGENASE activity in erythrocytes, leading to hemolytic anemia.	3.09	1	0
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.	5.6	3	2
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)	2.41	2	0
Parasitemia The presence of parasites (especially malarial parasites) in the blood. (Dorland, 27th ed)	4.37	2	2
Acute Disease Disease having a short and relatively severe course.	3.4	1	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.42	2	0
Adverse Drug Event [description not available]	3.41	1	1
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	3.41	1	1
Plasmodium vivax Malaria [description not available]	4.37	2	2
Malaria, Vivax Malaria caused by PLASMODIUM VIVAX. This form of malaria is less severe than MALARIA, FALCIPARUM, but there is a higher probability for relapses to occur. Febrile paroxysms often occur every other day.	4.37	2	2
Methemoglobinemia The presence of methemoglobin in the blood, resulting in cyanosis. A small amount of methemoglobin is present in the blood normally, but injury or toxic agents convert a larger proportion of hemoglobin into methemoglobin, which does not function reversibly as an oxygen carrier. Methemoglobinemia may be due to a defect in the enzyme NADH methemoglobin reductase (an autosomal recessive trait) or to an abnormality in hemoglobin M (an autosomal dominant trait). (Dorland, 27th ed)	2.39	2	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	1.97	1	0

bulaquine

Description

Cross-References

Synonyms (21)

Research Excerpts

Toxicity

Pharmacokinetics

Drug Classes (1)

Bioassays (3)

Research

Studies (21)

Study Types

bulaquine

Description

Cross-References

Synonyms (21)

Research Excerpts

Toxicity

Pharmacokinetics

Drug Classes (1)

Bioassays (3)

Research

Studies (21)

Study Types

Related Drugs (8)

Related Conditions (16)