Compounds > wr 99210
Page last updated: 2024-11-07

wr 99210

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Description

BRL 6231: RN given refers to parent cpd; NM & N1 refer to HCl; synonym BRL 51084 refers to (mono-HBr); structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID121750
CHEMBL ID129788
SCHEMBL ID8635467
MeSH IDM0048479

Synonyms (34)

Synonym
WRA ,
6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine
1,3,5-triazine-2,4-diamine, 1,6-dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-
wr99210
brl 6231 (*monohydrogen chloride*)
2,2-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-4,6-diamine
wr-99209 (*hydrogen bromide*)
6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine
wr-99210
4,6-diamino-1,2-dihydro-2,2-dimethyl-1-[(2,4,5-trichlorophenoxy)propyloxy]-1,3,5-triazine
1-(2',4',5'-trichlorophenoxypropoxy)-1,2-dihydro-2,2-dimethyl-4,6-diamino-s-triazine
brl 6231
brn 0629517
1,3,5-triazine-2,4-diamine, 1,6-dihydro-6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)propoxy)-
wr-99,210
wr 99210
1,6-dihydro-6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)propoxy)-1,3,5-triazine-2,4-diamine, monohydrochloride
1,6-dihydro-6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)-propoxy)-1,3,5-triazine-2 ,4-diamine
chembl129788 ,
bdbm18793
DB08734
47326-86-3
SCHEMBL8635467
1,6-dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine
4-imino-6,6-dimethyl-5-[3-(2,4,5-trichlorophenoxy)propoxy]-1h-1,3,5-triazin-2-amine
6,6-dimethyl-1-(3-(2,4,5-trichlorophenoxy)propoxy)-1,6-dihydro-1,3,5-triazine-2,4-diamine
Q27467334
HY-116387
CS-0065315
MS-26639
6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazinane-2,4-diimine
DTXSID30952947
XBA32686
AKOS040742826

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" The in vitro activities of WR99210 alone and in combination with a fixed concentration of dapsone (0."( Enhanced in vitro activity of WR99210 in combination with dapsone against Mycobacterium avium complex.
Cynamon, MH; DeStefano, MS; Shah, LM, 1996)		0.29

Dosage Studied

ExcerptRelevanceReference
" Four monkeys were orally dosed with 40 mg/kg/day of WR250417 over three days (-1, 0, and +1)."( Evaluation of WR250417 (a proguanil analog) for causal prophylactic activity in the Plasmodium cynomolgi-Macaca mulatta model.
Corcoran, KD; Edstein, MD; Hansukjariya, P; Ngampochjana, M; Rieckmann, KH; Sattabongkot, J; Shanks, GD; Webster, HK, 1994)		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)
Dihydrofolate reductaseHomo sapiens (human)Ki7.30390.00000.37564.9000AID1737539; AID518563
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K1Ki0.00030.00000.43696.6645AID1797769; AID238767
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum 3D7IC50 (µMol)0.09000.09001.28502.4800AID373640
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum 3D7Ki0.29230.00090.14660.2923AID373625
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
tetrahydrobiopterin biosynthetic processDihydrofolate reductaseHomo sapiens (human)
one-carbon metabolic processDihydrofolate reductaseHomo sapiens (human)
negative regulation of translationDihydrofolate reductaseHomo sapiens (human)
axon regenerationDihydrofolate reductaseHomo sapiens (human)
response to methotrexateDihydrofolate reductaseHomo sapiens (human)
dihydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate biosynthetic processDihydrofolate reductaseHomo sapiens (human)
folic acid metabolic processDihydrofolate reductaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityDihydrofolate reductaseHomo sapiens (human)
regulation of removal of superoxide radicalsDihydrofolate reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
mRNA regulatory element binding translation repressor activityDihydrofolate reductaseHomo sapiens (human)
mRNA bindingDihydrofolate reductaseHomo sapiens (human)
dihydrofolate reductase activityDihydrofolate reductaseHomo sapiens (human)
folic acid bindingDihydrofolate reductaseHomo sapiens (human)
NADPH bindingDihydrofolate reductaseHomo sapiens (human)
sequence-specific mRNA bindingDihydrofolate reductaseHomo sapiens (human)
NADP bindingDihydrofolate reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolDihydrofolate reductaseHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (112)

Assay IDTitleYearJournalArticle
AID559549Antimalarial activity against Plasmodium falciparum Kenyan isolates by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID373627Inhibition of WR99210-resistant form-3 Plasmodium falciparum N51I, C59R, N108T, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373628Inhibition of WR99210-resistant form-1 Plasmodium falciparum I51N, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373645Ratio of IC50 for pyrimethamine-resistant form-1 Plasmodium falciparum N51I, C59R, S108N, I164L, D187A mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1412528Oral bioavailability in Sprague-Dawley rat at 10 mg/kg administered via gavage2018MedChemComm, Mar-01, Volume: 9, Issue:3
Recent updates in the discovery and development of novel antimalarial drug candidates.
AID768487Antimalarial activity against trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as growth inhibition after 5 hrs by SYBR Green-I fluorescence assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID1145675Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID576705Ratio of IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S117N mutant to IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID576699Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145676Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 to IC50 for sensitive Lactobacillus casei ATCC 74691977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID373626Inhibition of pyrimethamine-resistant form-1 Plasmodium falciparum N51I, C59R, S108N, I164L, D187A mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1145681Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth in presence of 0.002 ug/ml folic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID560258Antimalarial activity against Plasmodium falciparum isolate Kil-164 expressing DHFR Ser108Asn, Asn51Ile, Cys59Arg and Ile164Leu quadruple mutant by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID373633Inhibition of WR99210-resistant form-A Plasmodium falciparum DHFR-TS I51N, C59R, N108S, L164I, D54N mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID518563Binding affinity to human recombinant DHFR expressed in Escherichia coli BL21(DE3) by competitive binding assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
AID1145688Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as active dose required to increase of 100% in mean survival time1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145680Antibacterial activity against sensitive Escherichia coli ATCC 10536 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID560256Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn and Cys59Arg or Ser108Asn and Asn51Ile double mutant by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID1737536Inhibition of Plasmodium falciparum DHFR N51I/C59R/S108N mutant expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID518564Selectivity ratio of Ki for human recombinant DHFR to Ki for wild type Plasmodium falciparum DHFR2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
AID158017In vitro antimalarial activity against Plasmodium falciparum W22001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
AID373639Inhibition of pyrimethamine-resistant form-1 Plasmodium falciparum N51I, C59R, S108N, I164L, D187A mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1737540Antimalarial activity against Plasmodium falciparum TM4/8.2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured after 20 hrs by radioactivity method2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID576701Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID768482Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in presence of 5 uM ALLN to IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in absence of ALLN2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID1737548Selectivity index, ratio of Ki for human DHFR expressed in Escherichia coli BL21 to Ki for Plasmodium falciparum DHFR N51I/C59R/S108N/I164L mutant expressed in Escherichia coli BL212020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID518565Selectivity ratio of Ki for recombinant Plasmodium falciparum V1/S DHFR S108N, N51I, C59R, I164L mutant to Ki for wild type Plasmodium falciparum DHFR2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
AID373643Ratio of IC50 for WR99210-resistant form-2 Plasmodium falciparum N51I, C59R, N108S, I164L mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373638Inhibition of WR99210-resistant form-3 Plasmodium falciparum N51I, C59R, N108T, I164L mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373641Inhibition of pyrimethamine-resistant form-3 Plasmodium falciparum N51I, C59R, S108N, I164L, I150V, N182I, N201D mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373632Inhibition of Plasmodium falciparum DHFR-TS QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1737553Inhibition of Plasmodium falciparum DHFR using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID576710Ratio of IC50 for Plasmodium falciparum TM91c235 harboring DHFR F57L, S58R, T61M, S117T mutant to IC50 for Plasmodium falciparum D62010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID768491Antimalarial activity against Plasmodium falciparum 3D7 infected in RBC assessed as growth inhibition after 48 hrs by SYBR Green-I fluorescence assay2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID159001In vitro antimalarial activity against Plasmodium falciparum K12001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
AID373634Inhibition of Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373631Inhibition of Plasmodium falciparum DHFR-TS QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1145673Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 to IC50 for sensitive Streptococcus faecium ATCC 80431977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1737537Inhibition of Plasmodium falciparum DHFR C59R/S108N/I164L mutant expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID768483Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in presence of 0.2 uM ALLN to IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in absence of ALLN2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID576702Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1737552Therapeutic index, ratio of IC50 for African green monkey Vero cells to IC50 for Plasmodium falciparum V1/S harboring DHFR N51I/C59R/S108N/I164L mutant2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID576706Ratio of IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L and S117N mutant to IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145682Antibacterial activity against chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 assessed as reduction in growth in presence of 0.002 ug/ml folic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145687Antibacterial activity against sensitive Escherichia coli ATCC 10536 assessed as reduction in growth in presence of p-aminobenzoic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID768469Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as nonviable parasite at 0.001 uM after 0.5 hrs by SYTO 61 staining-based flow cytometric analysis relative to untreated control2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID1629461Antimalarial activity against chloroquine/mefloquine-sensitive Plasmodium falciparum 3D7 infected-erythrocytes assessed as parasite growth inhibition after 48 to 54 hrs by SYBR green 1-based replication method2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Parallel inhibition of amino acid efflux and growth of erythrocytic Plasmodium falciparum by mefloquine and non-piperidine analogs: Implication for the mechanism of antimalarial action.
AID1145686Antibacterial activity against chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 assessed as reduction in growth in presence of 0.001 ug/ml folinic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1737545Antimalarial activity against Plasmodium falciparum V1/S harboring DHFR N51I/C59R/S108N/I164L mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measu2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID576700Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID768468Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as nonviable parasite at 0.0002 uM after 0.5 hrs by SYTO 61 staining-based flow cytometric analysis relative to untreated control2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID560257Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn, Asn51Ile and Cys59Arg triple mutant by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID518562Binding affinity to recombinant Plasmodium falciparum V1/S DHFR S108N, N51I, C59R, I164L mutant by competitive binding assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
AID248852In vitro antimalarial activity for DHFR wild-type, chloroquine and pyrimethamine-resistant Plasmodium falciparum W22005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
AID768457Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 0.001 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated co2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID248853In vitro antimalarial activity for DHFR wild-type, chloroquine and pyrimethamine-sensitive Plasmodium falciparum D62005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
AID1145679Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 to IC50 for sensitive Pediococcus cerevisiae ATCC 8081977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1737539Inhibition of human DHFR expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1737538Inhibition of Plasmodium falciparum DHFR N51I/C59R/S108N/I164L mutant expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID373642Ratio of IC50 for WR99210-resistant form-1 Plasmodium falciparum I51N, C59R, N108S, I164L mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID576698Antimalarial activity against Plasmodium falciparum TM91c235 harboring DHFR F57L, S58R, T61M, S117T mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145671Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID373635Ratio of IC50 for WR99210-resistant form-A Plasmodium falciparum DHFR-TS I51N, C59R, N108S, L164I, D54N mutant to IC50 for Plasmodium falciparum DHFR-TS QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID559547Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum V1S expressing DHFR quadruple mutant with point mutations at codons 108, 51, 59 and 164 gene by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID373644Ratio of IC50 for WR99210-resistant form-3 Plasmodium falciparum N51I, C59R, N108T, I164L mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373629Inhibition of Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1453043Apparent permeability across apical to basolateral side in human Caco2 cells at 50 uM after 90 mins by LC-MS/MS method2017European journal of medicinal chemistry, Jul-28, Volume: 135Guanylthiourea derivatives as potential antimalarial agents: Synthesis, in vivo and molecular modelling studies.
AID518561Binding affinity to wild type Plasmodium falciparum DHFR by competitive binding assay2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
AID1145677Antibacterial activity against sensitive Pediococcus cerevisiae ATCC 808 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1453044Oral bioavailability in Sprague-Dawley rat at 10 mg/kg, administered via gavage2017European journal of medicinal chemistry, Jul-28, Volume: 135Guanylthiourea derivatives as potential antimalarial agents: Synthesis, in vivo and molecular modelling studies.
AID1737551Therapeutic index, ratio of IC50 for African green monkey Vero cells to IC50 for Plasmodium falciparum K1CB1 harboring DHFR C59R/S108T mutant2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID576707Ratio of IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R and S117N mutant to IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID238767Inhibition constant against Plasmodium falciparum dihydrofolate reductase2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
AID576709Ratio of IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L, S58R, T61M, S117T mutant to IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145684Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth in presence of 0.001 ug/ml folic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1737543Antimalarial activity against Plasmodium falciparum W2 harboring DHFR N51I/C59R/S108N mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured afte2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1145672Antibacterial activity against chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID559548Antimalarial activity against pyrimethamine-sensitive Plasmodium falciparum 3D7 expressing wild type DHFR by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
AID1811397Selectivity index, ratio of IC50 for cytotoxicity against African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma brucei rhodesiense STI B9002021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of tetrahydroisoquinoline derivatives against Trypanosoma brucei rhodesiense.
AID373648Inhibition of WR99210-resistant form-2 Plasmodium falciparum N51I, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373646Ratio of IC50 for pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1737549Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID768455Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs to IC50 for Plasmodium falciparum 3D7 infected in RBC after 48 hrs2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID1145678Antibacterial activity against chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1737541Antimalarial activity against Plasmodium falciparum T9/94 RC17 harboring DHFR A16V/S108T mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured a2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID373636Inhibition of WR99210-resistant form-1 Plasmodium falciparum I51N, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1737546Selectivity index, ratio of Ki for human DHFR expressed in Escherichia coli BL21 to Ki for Plasmodium falciparum DHFR expressed in Escherichia coli BL212020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1737544Antimalarial activity against Plasmodium falciparum CsI-2 harboring DHFR C59R/S108N/I164L mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured 2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1737542Antimalarial activity against Plasmodium falciparum K1CB1 harboring DHFR C59R/S108T mutant infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 20 hrs followed by [3H]-hypoxanthine addition measured after 2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1629462Antimalarial activity against chloroquine/mefloquine-sensitive Plasmodium falciparum W2 assessed as parasite growth inhibition by [3H]hypoxanthine incorporation assay2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Parallel inhibition of amino acid efflux and growth of erythrocytic Plasmodium falciparum by mefloquine and non-piperidine analogs: Implication for the mechanism of antimalarial action.
AID1145674Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145683Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction in growth in presence of 0.001 ug/ml folic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1629463Antimalarial activity against trophozoite stage of Plasmodium falciparum 3D7 infected-erythrocytes assessed as reduction in Leu efflux after 4 hrs by UPLC method2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Parallel inhibition of amino acid efflux and growth of erythrocytic Plasmodium falciparum by mefloquine and non-piperidine analogs: Implication for the mechanism of antimalarial action.
AID1737550Therapeutic index, ratio of IC50 for African green monkey Vero cells to IC50 for Plasmodium falciparum TM4/8.22020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1737547Selectivity index, ratio of Ki for human DHFR expressed in Escherichia coli BL21 to Ki for Plasmodium falciparum DHFR double mutant expressed in Escherichia coli BL212020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID373637Inhibition of WR99210-resistant form-2 Plasmodium falciparum N51I, C59R, N108S, I164L mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID373625Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID576703Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R, T61M and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145685Antibacterial activity against sensitive Pediococcus cerevisiae ATCC 808 assessed as reduction in growth in presence of 0.001 ug/ml folinic acid1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID373647Ratio of IC50 for pyrimethamine-resistant form-3 Plasmodium falciparum N51I, C59R, S108N, I164L, I150V, N182I, N201D mutant to IC50 for Plasmodium falciparum DHFR QM template N51I, C59R, S108N, I164L mutant2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID576697Antimalarial activity against Plasmodium falciparum D6 infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1737535Inhibition of Plasmodium falciparum DHFR C59R/S108T mutant expressed in Escherichia coli BL21 using DHF as substrate by spectrophotometric analysis2020European journal of medicinal chemistry, Jun-01, Volume: 195Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.
AID1811395Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition measured after 72 hrs by alamar blue dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of tetrahydroisoquinoline derivatives against Trypanosoma brucei rhodesiense.
AID576704Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR F57L, S58R, T61M, S117T mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID1145689Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as dose required to survivors for period of 60 days1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID373624Inhibition of pyrimethamine-resistant form-3 Plasmodium falciparum N51I, C59R, S108N, I164L, I150V, N182I, N201D mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1811396Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Synthesis and evaluation of tetrahydroisoquinoline derivatives against Trypanosoma brucei rhodesiense.
AID373630Inhibition of WR99210-resistant form-A Plasmodium falciparum DHFR-TS I51N, C59R, N108S, L164I, D54N mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID576708Ratio of IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R, T61M and S117N mutant to IC50 for Plasmodium falciparum D6 harboring Plasmodium vivax wild type DHFR2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
AID768456Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 0.0002 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated c2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity.
AID373640Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3)2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
AID1797769Antimalarial Testing In Vitro (IC50) and Measurement of Inhibition Constant (Ki) from Article 10.1038/nsb921: \\Insights into antifolate resistance from malarial DHFR-TS structures.\\2003Nature structural biology, May, Volume: 10, Issue:5
Insights into antifolate resistance from malarial DHFR-TS structures.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (58)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (12.07)18.7374
1990's11 (18.97)18.2507
2000's25 (43.10)29.6817
2010's12 (20.69)24.3611
2020's3 (5.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.60

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 Index10.60 (24.57)
Research Supply Index4.09 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (1.69%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other58 (98.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
histamine
[no description available]		1.9510aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		1.9710aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.0810hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
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.		3.3770aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
cycloleucine
Cycloleucine: An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.. 1-aminocyclopentanecarboxylic acid : A non-proteinogenic alpha-amino acid that is cyclopentane substituted at position 1 by amino and carboxy groups.		1.9510non-proteinogenic alpha-amino acidEC 2.5.1.6 (methionine adenosyltransferase) inhibitor
dapsone
[no description available]		2.6630substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug
ellipticine
ellipticine : A organic heterotetracyclic compound that is pyrido[4,3-b]carbazole carrying two methyl substituents at positions 5 and 11.		2.3110indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound;
polycyclic heteroarene		antineoplastic agent;
plant metabolite
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		2.4220aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		2.0210nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
gentamicin
Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.		2.0210
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		2.0110carbohydrazideantitubercular agent;
drug allergen
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		1.9510catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
mefloquine hydrochloride
[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4.		2.0510organofluorine compound;
piperidines;
quinolines;
secondary alcohol
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.3110aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
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.		2.3620aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
pyrimethamine
Maloprim: contains above 2 cpds		4.68280aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		2.3620pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		1.9810isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfathiazole
Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position.		1.95101,3-thiazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		2.6830aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		2.4320
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		1.9510alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		1.9510imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
thymidine
[no description available]		2.0710pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
methylene blue
Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.		2.0810organic chloride saltacid-base indicator;
antidepressant;
antimalarial;
antimicrobial agent;
antioxidant;
cardioprotective agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 4.6.1.2 (guanylate cyclase) inhibitor;
fluorochrome;
histological dye;
neuroprotective agent;
physical tracer
methionine
Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.		2.110aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid		antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical
hexachloro-4-xylene
hexachloro-4-xylene: structure		1.9510
ornithine
Ornithine: An amino acid produced in the urea cycle by the splitting off of urea from arginine.. ornithine : An alpha-amino acid that is pentanoic acid bearing two amino substituents at positions 2 and 5.		2.0510non-proteinogenic L-alpha-amino acid;
ornithine		algal metabolite;
hepatoprotective agent;
mouse metabolite
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0310erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
sulfalene
Sulfalene: Long-acting plasma-bound sulfonamide used for respiratory and urinary tract infections and also for malaria.		1.9510pyrazines;
sulfonamide antibiotic;
sulfonamide
cycloguanil
cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.		4.45220triazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
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.		2.0310pyrimidines;
sulfonamide		antibacterial drug;
antimalarial
clopidol
pharmcoccide: Russian drug; no other info available 1/1/79		1.9510chloropyridine
4,6-diamino-2,2-dimethyl-1,2-dihydro-1-phenyl-s-triazine
4,6-diamino-2,2-dimethyl-1,2-dihydro-1-phenyl-s-triazine: structure in first source		2.0210
menoctone
[no description available]		2.3620
etoprine
etoprine: do not confuse with 3,5-dicarbethoxy-2,6-dimethyl-4-ethyl-1,4-dihydropyridine, also called DDEP		2.0210
wr 30090
WR 30090: RN given refers to parent cpd without isomeric designation; structure		1.9510
halofantrine
halofantrine: used in treatment of mild to moderate acute malaria		2.3820phenanthrenes
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		2.1310[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
chloroquine diphosphate
[no description available]		1.9610
fanasil, pyrimethamine drug combination
fanasil, pyrimethamine drug combination: combination drug containing fanasil & pyrimethamine		2.0310
clociguanil
clociguanil: RN given refers to parent cpd; structure		3.0850
2,4-diamino-5-phenyl-6-methylpyrimidine
2,4-diamino-5-phenyl-6-methylpyrimidine: analog of pyrimethamine; structure		2.0210
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.		2.4220hydroxy-1,2-naphthoquinone
pam 1392
[no description available]		1.9510
wr 158122
WR 158122: structure		1.9510
antibiotic g 418
antibiotic G 418: from Micromonospora rhodorangea		2.0210
methotrexate
[no description available]		3.0950dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
wr 194965
WR 194965: structure given in first source		1.9710
talotrexin
N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine: RN refers to (S)-isomer		2.0510
o 129
O 129: vibriostatic. 2,4-diamino-6,7-diisopropylpteridine : A member of the class of pteridines that is pteridine in which the hydrogens at positions 2 and 4 are replaced by amino groups, whilst those at positions 6 and 7 are replaced by isopropyl groups.. vibriostatic agent : Any compound that inhibits the growth of bacteria of the genus Vibrio.		1.9510primary amino compound;
pteridines		antifolate;
vibriostatic agent
puromycin
[no description available]		210puromycinsantiinfective agent;
antimicrobial agent;
antineoplastic agent;
EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor;
EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor;
nucleoside antibiotic;
protein synthesis inhibitor
5-carbethoxy-2-thiouracil
5-carbethoxy-2-thiouracil: structure in first source		1.9510
enpiroline
enpiroline: structure		1.9710
quinine
[no description available]		2.3620cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		2.3720
3-amino-1-methyl-5h-pyrido(4,3-b)indole
3-amino-1-methyl-5H-pyrido(4,3-b)indole: structure		2.0210pyridoindole
proguanil
Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells.		4.3190biguanides;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		2.4720artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine
1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine: structure		1.9510
ps 15
PS 15: structure given in first source; inhibitor of tetrahydrofolate dehydrogenase		3.3870
alpha-(2-piperidyl)-3,6-bis(trifluoromethyl)-9-phenanthrenemethanol
alpha-(2-piperidyl)-3,6-bis(trifluoromethyl)-9-phenanthrenemethanol: structure		1.9610
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.		2.3720
s-adenosylmethionine
(R)-S-adenosyl-L-methionine : An S-adenosyl-L-methionine that has R-configuration.. S-adenosyl-L-methionine zwitterion : A zwitterionic tautomer of S-adenosyl-L-methionine arising from shift of the proton from the carboxy group to the amino group.. (R)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has R-configuration; major species at pH 7.3.. (S)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has S-configuration; major species at pH 7.3.. S-adenosyl-L-methionine : A sulfonium compound that is the S-adenosyl derivative of L-methionine. It is an intermediate in the metabolic pathway of methionine.		2.110organic cation;
sulfonium compound		coenzyme;
cofactor;
human metabolite;
micronutrient;
Mycoplasma genitalium metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
piperidines
Piperidines: A family of hexahydropyridines.		1.9610
6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1h)-one
6-Chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1H)-one: structure in first source		3.2710
isoatriplicolide tiglate
isoatriplicolide tiglate: from Paulownia coreana; structure in first source		2.3110
sj733
SJ733: antimalarial; structure in first source		3.2710
blasticidin s
blasticidin S: RN given refers to (S)-isomer; structure. blasticidin S : A blasticidin that is an antibiotic obtained from Streptomyces griseochromogene.		2.4620
levoleucovorin
Levoleucovorin: A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.. (6S)-5-formyltetrahydrofolic acid : The pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid.		2105-formyltetrahydrofolic acidantineoplastic agent;
metabolite
hypoxanthine
[no description available]		1.9910nucleobase analogue;
oxopurine;
purine nucleobase		fundamental metabolite
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		2.4420folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.0110cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ganciclovir
[no description available]		2.42202-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
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.		2.6630
ConditionIndicatedRelationship StrengthStudiesTrials
Infections, Plasmodium
[description not available]		03.5990
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.		03.5990
Plasmodium falciparum Malaria
[description not available]		03.2660
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.		03.2660
Babesia Infection
[description not available]		02.1110
Bovine Diseases
[description not available]		02.1110
Koch's Disease
[description not available]		02.0510
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		02.0510
P carinii Infection
[description not available]		02.0110
Pneumocystis Infections
Infections with species in the genus PNEUMOCYSTIS, a fungus causing interstitial plasma cell pneumonia (PNEUMONIA, PNEUMOCYSTIS) and other infections in humans and other MAMMALS. Immunocompromised patients, especially those with AIDS, are particularly susceptible to these infections. Extrapulmonary sites are rare but seen occasionally.		02.0110
Delayed Hypersensitivity
[description not available]		01.9610
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		01.9810
Leucocythaemia
[description not available]		01.9910
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		01.9910