Page last updated: 2024-08-20

cycloguanil and pyrimethamine

cycloguanil has been researched along with pyrimethamine in 101 studies

Research

Studies (101)

TimeframeStudies, this research(%)All Research%
pre-199020 (19.80)18.7374
1990's22 (21.78)18.2507
2000's39 (38.61)29.6817
2010's19 (18.81)24.3611
2020's1 (0.99)2.80

Authors

AuthorsStudies
Genther, CS; Smith, CS1
Coats, EA; Genther, CS; Hansch, C; Selassie, CD; Strong, CD1
Chu, V; Elslager, EF; Hess, C; Johnson, J; Ortwine, D; Werbel, LM1
Queener, SF1
Chan, C; Dascombe, MJ; Douglas, KT; Hyde, JE; McKie, JH; Read, M; Roser, SA; Sirawaraporn, W; Yates, R; Yuthavong, Y1
Jomaa, H; Mitsch, A; Schlitzer, M; Wiesner, J; Wissner, P1
Ager, AL; Bliss, RA; Canfield, CJ; Jacobus, DP; Jensen, NP; Kotecka, BM; Rieckmann, KH; Terpinski, J1
Jomaa, H; Kettler, K; Schlitzer, M; Wiesner, J1
Jomaa, H; Krämer, O; Mitsch, A; Schlitzer, M; Wiesner, J; Wissner, P1
Jomaa, H; Kettler, K; Ortmann, R; Sakowski, J; Schlitzer, M; Wiesner, J1
Fucik, K; Jomaa, H; Kettler, K; Ortmann, R; Sakowski, J; Schlitzer, M; Wiesner, J1
Chitnumsub, P; Kamchonwongpaisan, S; Sirawaraporn, W; Taylor, P; Vanichtanankul, J; Walkinshaw, MD; Yuthavong, Y; Yuvaniyama, J1
Jomaa, H; Mitsch, A; Schlitzer, M; Wiesner, J1
Ferrari, AM; Pacchioni, S; Parenti, MD; Rastelli, G; Sirawaraporn, R; Sirawaraporn, W1
Charoensetakul, N; Kamchonwongpaisan, S; Lowe, G; Ponsinet, R; Quarrell, R; Sirawaraporn, W; Tarnchompoo, B; Vanichtanankul, J; Vilaivan, T; Yuthavong, Y1
Ferrari, AM; Pacchioni, S; Parenti, MD; Rastelli, G1
Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; O'Neil, MT; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, PL; Yang, YS1
Bertaux, L; Bogreau, H; Bouchiba, H; Garnotel, E; Kraemer, P; Parzy, D; Pradines, B; Rogier, C; Savini, H; Simon, F1
García-Mera, X; González-Díaz, H; Prado-Prado, FJ1
Brun, R; Chitnumsub, P; Dartois, V; Diagana, TT; Goh, A; Kamchonwongpaisan, S; Keller, TH; Kiara, SM; Lakshminarayana, SB; Ma, NL; Maneeruttanarungroj, C; Nzila, A; Rottmann, M; Taweechai, S; Weaver, M; Wittlin, S; Wong, J; Yeung, BK; Yuthavong, Y; Zou, B1
Adams, JH; Auliff, AM; Cheng, Q; O'Neil, MT1
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y1
Biamonte, MA; Le Roch, KG; Wanner, J1
Azas, N; Basmaciyan, L; Cohen, A; Crozet, MD; Dallemagne, P; Deharo, E; Dumètre, A; Hutter, S; Laget, M; Lancelot, JC; Lesnard, A; Lorthiois, A; Mazier, D; Paloque, L; Rathelot, P; Rault, S; Sibley, CH; Suzanne, P; Valentin, A; Vanelle, P; Verhaeghe, P1
Cheenpracha, S; Jaidee, A; Kamchonwongpaisan, S; Laphookhieo, S; Promchai, T; Pyne, SG; Rattanajak, R; Ritthiwigrom, T; Trisuwan, K1
Cichero, E; Espinoza, S; Gainetdinov, RR; Tonelli, M1
Cichero, E; Costi, MP; Gazzarrini, S; Loddo, R; Moroni, A; Naesens, L; Santucci, M; Tasso, B; Tonelli, M1
Aguiar, ACC; Berlinck, RGS; Bertonha, AF; Costa, TR; de Souza, GE; Ferreira, AG; Gadelha, FR; Grazzia, N; Guido, RVC; Hajdu, E; Miguel, DC; Oliva, G; Parra, LLL; Romo, D; Severo, IRM1
Gyang, FN; Peterson, DS; Wellems, TE1
Bjorkman, A; Flacks, H; Hanson, AP; Hogh, B; Petersen, E1
Cowman, AF; Foote, SJ; Galatis, D1
Milhous, WK; Peterson, DS; Wellems, TE1
Booth, RG; Hansch, C; Neal, RA; Santi, DV; Sertsrivanich, R; Sirawaraporn, W1
Barutwanayo, M; Coosemans, MH; Gryseels, B; Onori, E; Otoul, C; Wéry, M1
Childs, GE; Lambros, C1
Koech, DK; Sixsmith, DG; Spencer, HC; Watkins, WW1
Howells, RE; Percy, M1
Bygbjerg, IC; Flachs, H1
Edstein, MD1
Barber, AM; Campbell, CC; Collins, WE; Nguyen-Dinh, P; Teklehaimanot, A1
Greenwood, BM; Panton, LJ1
Bent, NS; Gilles, HM; Howells, RE1
Schapira, A1
Chulay, JD; Sixsmith, DG; Spencer, HC; Watkins, WM1
Chulay, JD; Sixsmith, DG; Watkins, WM1
Rossan, RN; Schmidt, LH1
Høiby, N; Kharazmi, A; Valerius, NH1
Howells, RE; Judge, BM1
Graham, NB; Howells, RE; Judge, BM; McNeill, ME1
Basco, LK; Eldin de Pécoulas, P; Le Bras, J; Mazabraud, A; Wilson, CM1
Abdallah, B; Basco, LK; Djé, MK; Eldin de Pécoulas, P; Le Bras, J; Mazabraud, A1
Basco, LK; Le Bras, J2
Basco, LK; Le Bras, J; Ramiliarisoa, O1
Basco, LK; de Pecoulas, PE; Le Bras, J; Wilson, CM1
Cowman, AF; Genton, B; Lorry, K; Reeder, JC; Rieckmann, KH; Wines, B1
Bhasin, VK; Nair, L1
Nguyen, DS; Nguyen, PD; Sköld, O; Swedberg, G; Zindrou, S1
Ang, HH; Chan, KL; Mak, JW1
Santi, DV; Sathitkul, T; Sirawaraporn, R; Sirawaraporn, W; Yuthavong, Y1
Christopherson, RI; Rieckmann, KH; Seymour, KK; Yeo, AE1
Santi, DV; Sirawaraporn, R; Sirawaraporn, W; Yongkiettrakul, S; Yuthavong, Y1
Mberu, EK; Nzila-Mounda, A; Plowe, CV; Sibley, CH; Watkins, WM; Winstanley, PA1
Reynolds, MG; Roos, DS1
Howard, V; Mookherjee, S; Nzila-Mouanda, A; Sibley, CH; Watkins, W1
Auparakkitanon, S; Chavalitshewinkoon-Petmitr, P; Pongvilairat, G; Wilairat, P1
Fusai, T; Mosnier, J; Parzy, D; Pradines, B; Rogier, C; Spiegel, A; Tall, A; Trape, JF1
Basco, LK; Ringwald, P1
Kamchonwongpaisan, S; Lowe, G; Quarrell, R; Rastelli, G; Sirawaraporn, W; Sompornpisut, P; Thebtaranonth, Y; Vilaivan, T; Yuthavong, Y1
Bhasin, V; Nair, L; Toteja, R1
de Alencastro, RB; Figueroa-Villar, JD; Santos-Filho, OA1
Hankins, EG; Sibley, CH; Warhurst, DC1
Delfino, RT; Figueroa-Villar, JD; Santos-Filho, OA1
Hastings, MD; Sibley, CH1
Liu, H; Yang, YM; Zhang, ZX1
Durand, R; Le Bras, J1
Ariey, F; Duchemin, JB; Harisoa, JL; Mauclere, P; Pietra, V; Rabarijaona, LP; Raharimalala, LA; Rakotomanana, F; Ranaivo, L; Randrianarivelojosia, M; Robert, V1
Charlieu, JP; Imwong, M; Leartsakulpanich, U; Letourneur, F; Looareesuwan, S; Pukrittayakamee, S; Rénia, L; Snounou, G; White, NJ1
Aubouy, A; Bakary, M; Deloron, P; Durand, R; Huart, V; Jafari, S; Le Bras, J; Mayombo, J; Migot-Nabias, F1
Bienzle, U; Ehrhardt, S; Jelinek, T; Mockenhaupt, FP; Muehlen, M; Otchwemah, R; Schreiber, J1
Hunt, SY; Rezvani, BB; Sibley, CH1
Kamchonwongpaisan, S; Tarnchompoo, B; Taweechai, S; Vanichtanankul, J; Yuthavong, Y; Yuvaniyama, J1
Chusacultanachai, S; Japrung, D; Wilairat, P; Yuthavong, Y; Yuvaniyama, J1
Jiang, S; McConkey, GA; McRobert, L; Stead, A1
Ang, HH; Cheang, HS; Mak, JW1
Anh, le N; Auliff, A; Bell, D; Chen, N; Cheng, Q; Gao, Q; Maguire, J; O'Neil, MT; Russell, B; Wilson, DW1
Chitnumsub, P; Kamchonwongpaisan, S; Taweechai, S; Vanichtanankul, J; Yuthavong, Y1
Chusacultanachai, S; Japrung, D; Leartsakulpanich, U; Yuthavong, Y1
Diriye, A; Kiara, S; Kokwaro, G; Masseno, V; Mwai, L; Nduati, E; Nzila, A; Ommeh, S1
Chishimba, S; Mharakurwa, S; Mkulama, MA; Rouse, P; Sikalima, J; Thuma, PE1
Borrmann, S; Kiara, SM; Masseno, V; Mwai, L; Nzila, A; Ochola, I; Okombo, J1
Adane, L; Bharatam, PV; Patel, DS1
Brown, KM; Costanzo, MS; Hartl, DL1
Imwong, M; Kongsaeree, P; Leartsakulpanich, U; Riangrungroj, P; Tirakarn, S; Yuthavong, Y1
Adams, JH; Auliff, AM; Balu, B; Chen, N; Cheng, Q; O'Neil, MT1
Blundell, TL; Dias, MV; Domingues, RR; Paes Leme, AF; Tyrakis, P1
Diakite, I; Hartl, DL; Ogbunugafor, CB; Weinreich, DM; Wylie, CS1
Corral, MG; Leroux, J; Mylne, JS; Stubbs, KA1
Blasco, B; Moon, RW; Sutherland, CJ; van Schalkwyk, DA1
Ittarat, W; Kongkasuriyachai, D; Leartsakulpanich, U; Leelayoova, S; Mungthin, M; Pornthanakasem, W; Suwandittakul, N; Tarnchompoo, B; Yuthavong, Y1
Hoarau, M; Kamchonwongpaisan, S; Srimongkolpithak, N; Vanichtanankul, J; Vitsupakorn, D; Yuthavong, Y1

Reviews

3 review(s) available for cycloguanil and pyrimethamine

ArticleYear
New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii.
    Journal of medicinal chemistry, 1995, Nov-24, Volume: 38, Issue:24

    Topics: Animals; Drug Design; Humans; Immunosuppression Therapy; Molecular Structure; Opportunistic Infections; Pneumonia, Pneumocystis; Structure-Activity Relationship

1995
Recent advances in malaria drug discovery.
    Bioorganic & medicinal chemistry letters, 2013, May-15, Volume: 23, Issue:10

    Topics: Animals; Antimalarials; Drug Discovery; Humans; Liver; Liver Transplantation; Malaria; Molecular Structure

2013
The mechanisms of resistance to antimalarial drugs in Plasmodium falciparum.
    Fundamental & clinical pharmacology, 2003, Volume: 17, Issue:2

    Topics: Africa; Animals; Antimalarials; Antimetabolites; Chloroquine; Drug Resistance; Drug Resistance, Multiple; Humans; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

2003

Trials

1 trial(s) available for cycloguanil and pyrimethamine

ArticleYear
Double-blind study to assess the efficacy of chlorproguanil given alone or in combination with chloroquine for malaria chemoprophylaxis in an area with Plasmodium falciparum resistance to chloroquine, pyrimethamine and cycloguanil.
    Transactions of the Royal Society of Tropical Medicine and Hygiene, 1987, Volume: 81, Issue:1

    Topics: Adolescent; Animals; Antimalarials; Child; Chloroquine; Clinical Trials as Topic; Double-Blind Method; Drug Resistance; Drug Therapy, Combination; Female; Humans; Malaria; Male; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1987

Other Studies

97 other study(ies) available for cycloguanil and pyrimethamine

ArticleYear
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
    Journal of medicinal chemistry, 1977, Volume: 20, Issue:2

    Topics: Animals; Antimalarials; Bacteria; Drug Resistance, Microbial; Escherichia coli; Folic Acid; Folic Acid Antagonists; Malaria; Mice; Plasmodium berghei; Triazines

1977
Quantitative structure-activity relationship of antifolate inhibition of bacteria cell cultures resistant and sensitive to methotrexate.
    Journal of medicinal chemistry, 1985, Volume: 28, Issue:12

    Topics: Biological Transport, Active; Chemical Phenomena; Chemistry; Drug Resistance, Microbial; Escherichia coli; Folic Acid Antagonists; Lacticaseibacillus casei; Mathematics; Methotrexate; Pyrimethamine; Pyrimidines; Structure-Activity Relationship; Triazines

1985
Synthesis and antimalarial effects of N2-aryl-N4-[(dialkylamino)alkyl]- and N4-aryl-N2-[(dialkylamino)alkyl]-2,4-quinazolinediamines.
    Journal of medicinal chemistry, 1981, Volume: 24, Issue:2

    Topics: Animals; Antimalarials; Chemical Phenomena; Chemistry; Drug Evaluation, Preclinical; Drug Resistance; Mice; Plasmodium berghei; Quinazolines; Structure-Activity Relationship

1981
Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria.
    Journal of medicinal chemistry, 1998, Apr-23, Volume: 41, Issue:9

    Topics: Animals; Antimalarials; Drug Design; Drug Resistance; Folic Acid Antagonists; Malaria; Male; Mice; Multienzyme Complexes; Mutation; Plasmodium berghei; Plasmodium falciparum; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase

1998
Structure-activity relationships of novel anti-malarial agents. Part 2: cinnamic acid derivatives.
    Bioorganic & medicinal chemistry letters, 2001, Feb-12, Volume: 11, Issue:3

    Topics: Animals; Antimalarials; Cinnamates; Combinatorial Chemistry Techniques; Inhibitory Concentration 50; Microbial Sensitivity Tests; Plasmodium falciparum; Structure-Activity Relationship

2001
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
    Journal of medicinal chemistry, 2001, Nov-08, Volume: 44, Issue:23

    Topics: Animals; Antimalarials; Drug Evaluation, Preclinical; Female; Folic Acid Antagonists; Guanidines; Malaria; Male; Mice; Plasmodium berghei; Plasmodium falciparum; Prodrugs; Proguanil; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2001
Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides.
    Bioorganic & medicinal chemistry letters, 2002, Feb-25, Volume: 12, Issue:4

    Topics: Amides; Animals; Antimalarials; Benzophenones; Cinnamates; Humans; Inhibitory Concentration 50; Phenylacetates; Plasmodium falciparum; Structure-Activity Relationship

2002
Structure-activity relationships of novel anti-malarial agents. Part 4: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides.
    Bioorganic & medicinal chemistry letters, 2002, Oct-07, Volume: 12, Issue:19

    Topics: Acrylamides; Animals; Antimalarials; Drug Resistance; Hydrogen Bonding; Indicators and Reagents; Plasmodium falciparum; Structure-Activity Relationship

2002
Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
    Bioorganic & medicinal chemistry letters, 2003, Feb-10, Volume: 13, Issue:3

    Topics: Acrylates; Animals; Antimalarials; Drug Resistance, Multiple; Erythrocytes; Furans; Humans; Indicators and Reagents; Plasmodium falciparum; Structure-Activity Relationship

2003
Structure-activity relationships of novel anti-malarial agents. Part 6: N-(4-arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
    Bioorganic & medicinal chemistry letters, 2003, May-05, Volume: 13, Issue:9

    Topics: Amides; Animals; Antimalarials; Benzophenones; Furans; Nitro Compounds; Plasmodium falciparum; Stereoisomerism; Structure-Activity Relationship

2003
Insights into antifolate resistance from malarial DHFR-TS structures.
    Nature structural biology, 2003, Volume: 10, Issue:5

    Topics: Amino Acid Sequence; Animals; Conserved Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Multienzyme Complexes; Plasmodium; Plasmodium falciparum; Protein Conformation; Sequence Alignment; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase

2003
Structure-activity relationships of novel anti-malarial agents. Part 7: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides with polar moieties.
    Bioorganic & medicinal chemistry letters, 2003, Jul-07, Volume: 13, Issue:13

    Topics: Acrylates; Alkyl and Aryl Transferases; Amides; Animals; Antimalarials; Enzyme Inhibitors; Farnesyltranstransferase; Furans; Hydrogen Bonding; Indicators and Reagents; Plasmodium falciparum; Structure-Activity Relationship

2003
Docking and database screening reveal new classes of Plasmodium falciparum dihydrofolate reductase inhibitors.
    Journal of medicinal chemistry, 2003, Jul-03, Volume: 46, Issue:14

    Topics: Animals; Antimalarials; Databases, Factual; Drug Design; Folic Acid Antagonists; Models, Molecular; Mutation; Plasmodium falciparum; Tetrahydrofolate Dehydrogenase

2003
Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.
    Journal of medicinal chemistry, 2004, Jan-29, Volume: 47, Issue:3

    Topics: Animals; Antimalarials; Cell Line; Chlorocebus aethiops; Drug Resistance; Folic Acid Antagonists; Humans; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2004
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach.
    Journal of medicinal chemistry, 2004, Aug-12, Volume: 47, Issue:17

    Topics: Aldehyde Reductase; Animals; Antimalarials; Binding Sites; Folic Acid Antagonists; Models, Molecular; Plasmodium falciparum; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase

2004
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
    Journal of medicinal chemistry, 2005, Apr-21, Volume: 48, Issue:8

    Topics: Animals; Antimalarials; Biguanides; Chromatography, Liquid; Drug Resistance; Folic Acid Antagonists; Humans; In Vitro Techniques; Mass Spectrometry; Microsomes, Liver; Plasmodium falciparum; Prodrugs; Structure-Activity Relationship; Triazines

2005
First case of emergence of atovaquone-proguanil resistance in Plasmodium falciparum during treatment in a traveler in Comoros.
    Antimicrobial agents and chemotherapy, 2008, Volume: 52, Issue:6

    Topics: Animals; Antimalarials; Atovaquone; Comoros; Drug Resistance; France; Genotype; Humans; Malaria, Falciparum; Male; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Travel; Treatment Failure

2008
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
    Bioorganic & medicinal chemistry, 2010, Mar-15, Volume: 18, Issue:6

    Topics: Antiparasitic Agents; Molecular Structure; Neural Networks, Computer; Parasitic Diseases; Quantitative Structure-Activity Relationship; Species Specificity; Thermodynamics

2010
Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Administration, Oral; Animals; Antimalarials; Biological Availability; Drug Resistance; Female; Folic Acid Antagonists; Humans; In Vitro Techniques; Malaria; Malaria, Falciparum; Male; Mice; Models, Molecular; Mutation; Parasitic Sensitivity Tests; Plasmodium berghei; Plasmodium falciparum; Pyrimethamine; Quinazolines; Rats; Rats, Wistar; Tetrahydrofolate Dehydrogenase

2010
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:9

    Topics: Animals; Folic Acid Antagonists; Multienzyme Complexes; Mutation; Parasitic Sensitivity Tests; Plasmodium falciparum; Plasmodium vivax; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection

2010
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
    Science (New York, N.Y.), 2011, Dec-09, Volume: 334, Issue:6061

    Topics: Animals; Antimalarials; Cell Line, Tumor; Drug Discovery; Drug Evaluation, Preclinical; Drug Resistance; Erythrocytes; Humans; Imidazoles; Liver; Malaria; Mice; Mice, Inbred BALB C; Molecular Structure; Piperazines; Plasmodium; Plasmodium berghei; Plasmodium falciparum; Plasmodium yoelii; Polymorphism, Single Nucleotide; Protozoan Proteins; Random Allocation; Small Molecule Libraries; Sporozoites

2011
Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium.
    European journal of medicinal chemistry, 2015, May-05, Volume: 95

    Topics: Animals; Antimalarials; Cell Proliferation; CHO Cells; Cricetinae; Cricetulus; Drug Discovery; Erythrocytes; Hep G2 Cells; Humans; Liver; Malaria; Male; Mice; Parasitemia; Plasmodium falciparum; Pyrimidines; Structure-Activity Relationship; Trophozoites

2015
Antimalarial Oxoprotoberberine Alkaloids from the Leaves of Miliusa cuneata.
    Journal of natural products, 2016, Apr-22, Volume: 79, Issue:4

    Topics: Alkaloids; Animals; Annonaceae; Antimalarials; Chlorocebus aethiops; Dose-Response Relationship, Drug; Humans; KB Cells; Malaria; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Plant Leaves; Plasmodium berghei; Plasmodium falciparum; Vero Cells

2016
Novel biguanide-based derivatives scouted as TAAR1 agonists: Synthesis, biological evaluation, ADME prediction and molecular docking studies.
    European journal of medicinal chemistry, 2017, Feb-15, Volume: 127

    Topics: Absorption, Physicochemical; Animals; Biguanides; Chemistry Techniques, Synthetic; Computer Simulation; Drug Design; Humans; Mice; Molecular Docking Simulation; Protein Conformation; Receptors, G-Protein-Coupled; Structure-Activity Relationship

2017
Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
    European journal of medicinal chemistry, 2017, Jul-28, Volume: 135

    Topics: Antiviral Agents; Crystallography, X-Ray; Dose-Response Relationship, Drug; Folic Acid Antagonists; Humans; Influenza A Virus, H1N1 Subtype; Influenza B virus; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Proguanil; Respiratory Syncytial Viruses; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2017
Isolation, Derivative Synthesis, and Structure-Activity Relationships of Antiparasitic Bromopyrrole Alkaloids from the Marine Sponge Tedania brasiliensis.
    Journal of natural products, 2018, 01-26, Volume: 81, Issue:1

    Topics: Alkaloids; Animals; Antimalarials; Antiparasitic Agents; Antiprotozoal Agents; Chagas Disease; Leishmania infantum; Leishmaniasis, Visceral; Parasitic Sensitivity Tests; Plasmodium falciparum; Porifera; Structure-Activity Relationship; Trypanosoma cruzi

2018
Plasmodium falciparum: rapid detection of dihydrofolate reductase mutations that confer resistance to cycloguanil and pyrimethamine.
    Experimental parasitology, 1992, Volume: 74, Issue:4

    Topics: Animals; Base Sequence; Drug Resistance; Molecular Sequence Data; Mutation; Plasmodium falciparum; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

1992
In vitro and in vivo susceptibility of Plasmodium falciparum isolates from Liberia to pyrimethamine, cycloguanil and chlorcycloguanil.
    Annals of tropical medicine and parasitology, 1990, Volume: 84, Issue:6

    Topics: Animals; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance; Humans; In Vitro Techniques; Liberia; Malaria; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1990
Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance.
    Proceedings of the National Academy of Sciences of the United States of America, 1990, Volume: 87, Issue:8

    Topics: Amino Acid Sequence; Animals; Base Sequence; DNA; Drug Resistance; Genes; Molecular Sequence Data; Oligonucleotide Probes; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

1990
Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria.
    Proceedings of the National Academy of Sciences of the United States of America, 1990, Volume: 87, Issue:8

    Topics: Amino Acid Sequence; Animals; Binding Sites; DNA; Drug Resistance; Humans; Malaria; Models, Structural; Molecular Structure; Mutation; Plasmodium falciparum; Proguanil; Protein Conformation; Pyrimethamine; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

1990
Selective inhibition of Leishmania dihydrofolate reductase and Leishmania growth by 5-benzyl-2,4-diaminopyrimidines.
    Molecular and biochemical parasitology, 1988, Volume: 31, Issue:1

    Topics: Animals; Antimalarials; Folic Acid Antagonists; Leishmania tropica; Proguanil; Pyrimethamine; Pyrimidines; Triazines; Trimethoprim

1988
Analogues of N-benzyloxydihydrotriazines: in vitro antimalarial activity against Plasmodium falciparum.
    Annals of tropical medicine and parasitology, 1986, Volume: 80, Issue:2

    Topics: Antimalarials; Chloroquine; Drug Resistance, Microbial; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1986
Response of Plasmodium falciparum to dihydrofolate reductase inhibitors in Malindi, Kenya.
    Transactions of the Royal Society of Tropical Medicine and Hygiene, 1986, Volume: 80, Issue:2

    Topics: Child; Drug Resistance, Microbial; Drug Therapy, Combination; Folic Acid Antagonists; Humans; Kenya; Malaria; Plasmodium falciparum; Proguanil; Pyrimethamine; Sulfadoxine; Sulfanilamides; Triazines

1986
The interaction of the naphthoquinone derivative menoctone and dihydrofolate reductase inhibitors on Plasmodium falciparum in vitro.
    Annals of tropical medicine and parasitology, 1986, Volume: 80, Issue:3

    Topics: Animals; Antiprotozoal Agents; Drug Interactions; Folic Acid Antagonists; Hypoxanthines; Naphthoquinones; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1986
Effect of oral proguanil on human lymphocyte proliferation.
    European journal of clinical pharmacology, 1986, Volume: 30, Issue:2

    Topics: Adult; Humans; Leukocyte Count; Leukocytes; Lymphocyte Activation; Lymphocytes; Phytohemagglutinins; Proguanil; Pyrimethamine; Thymidine; Time Factors; Triazines

1986
Simultaneous measurement of proguanil and cycloguanil in human plasma by high-performance liquid chromatography.
    Journal of chromatography, 1986, Jul-11, Volume: 380, Issue:1

    Topics: Chemical Phenomena; Chemistry; Chromatography, High Pressure Liquid; Humans; Proguanil; Pyrimethamine; Spectrophotometry, Ultraviolet; Triazines

1986
Evaluation of sporontocidal compounds using Plasmodium falciparum gametocytes produced in vitro.
    The American journal of tropical medicine and hygiene, 1985, Volume: 34, Issue:3

    Topics: Anopheles; Antimalarials; Drug Resistance, Microbial; Humans; Plasmodium falciparum; Primaquine; Proguanil; Pyrimethamine; Triazines

1985
In vitro sensitivity of Plasmodium falciparum to chlorcycloguanil in The Gambia.
    Transactions of the Royal Society of Tropical Medicine and Hygiene, 1985, Volume: 79, Issue:4

    Topics: Animals; Antimalarials; Dose-Response Relationship, Drug; Gambia; Microbial Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1985
A comparison of the pyrimethamine and cycloguanil sensitivities of the pre-erythrocytic and erythrocytic stages of drug-sensitive and -resistant strains of Plasmodium yoelii.
    Annals of tropical medicine and parasitology, 1985, Volume: 79, Issue:3

    Topics: Animals; Dose-Response Relationship, Drug; Drug Resistance, Microbial; Malaria; Male; Mice; Plasmodium; Proguanil; Pyrimethamine; Triazines

1985
Concomitant resistance to pyrimethamine and cycloguanil of chloroquine-resistant falciparum malaria from East Africa: an in vitro study of 12 isolates.
    Transactions of the Royal Society of Tropical Medicine and Hygiene, 1984, Volume: 78, Issue:3

    Topics: Africa, Eastern; Chloroquine; Drug Resistance, Microbial; Humans; Malaria; Microbial Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1984
In vitro antimalarial activity of tetrahydrofolate dehydrogenase inhibitors.
    The American journal of tropical medicine and hygiene, 1984, Volume: 33, Issue:5

    Topics: Animals; Culture Media; Folic Acid Antagonists; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1984
The activity of proguanil and its metabolites, cycloguanil and p-chlorophenylbiguanide, against Plasmodium falciparum in vitro.
    Annals of tropical medicine and parasitology, 1984, Volume: 78, Issue:3

    Topics: Animals; Biguanides; Chloroquine; Microbial Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1984
Activities of respository preparations of cycloguanil pamoate and 4,4'-diacetyldiaminodiphenylsulfone, alone and in combination, against infections with Plasmodium cynomolgi in rhesus monkeys.
    Antimicrobial agents and chemotherapy, 1984, Volume: 26, Issue:5

    Topics: Acedapsone; Animals; Antimalarials; Dapsone; Drug Combinations; Drug Resistance, Microbial; Macaca mulatta; Malaria; Particle Size; Plasmodium falciparum; Plasmodium vivax; Proguanil; Pyrimethamine; Time Factors; Triazines

1984
Effect of antimalarial drugs on human neutrophil chemotaxis in vitro.
    Acta pathologica, microbiologica, et immunologica Scandinavica. Section C, Immunology, 1983, Volume: 91, Issue:4

    Topics: Antimalarials; Chemotaxis, Leukocyte; Chloroquine; Drug Combinations; Humans; Neutrophils; Proguanil; Pyrimethamine; Quinine; Sulfadoxine; Tetracycline; Triazines

1983
Sustained-release implants in the chemotherapy of experimental rodent malaria I. A comparison of the effects of some antimalarials in polydimethylsiloxane matrices.
    Annals of tropical medicine and parasitology, 1981, Volume: 75, Issue:5

    Topics: Animals; Antimalarials; Chloroquine; Dimethylpolysiloxanes; Drug Implants; Malaria; Male; Mefloquine; Mice; Mice, Inbred Strains; Naphthoquinones; Piperidines; Plasmodium berghei; Primaquine; Proguanil; Pyrimethamine; Quinolines; Silicone Elastomers; Sulfadiazine; Triazines

1981
Sustained-release implants in the chemotherapy of experimental rodent malaria II. The effects of sulphadiazine, pyrimethamine and cycloguanil in biodegradable polymer matrices.
    Annals of tropical medicine and parasitology, 1981, Volume: 75, Issue:5

    Topics: Animals; Biodegradation, Environmental; Drug Implants; Malaria; Male; Mice; Mice, Inbred Strains; Plasmodium berghei; Proguanil; Pyrimethamine; Sulfadiazine; Triazines

1981
Point mutations in the dihydrofolate reductase-thymidylate synthase gene and pyrimethamine and cycloguanil resistance in Plasmodium falciparum.
    Molecular and biochemical parasitology, 1995, Volume: 69, Issue:1

    Topics: Amino Acid Sequence; Animals; Base Sequence; Drug Resistance, Multiple; Humans; Malaria, Falciparum; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

1995
Plasmodium falciparum: detection of antifolate resistance by mutation-specific restriction enzyme digestion.
    Experimental parasitology, 1995, Volume: 80, Issue:3

    Topics: Animals; Base Sequence; Codon; DNA Primers; Drug Resistance; Genes, Protozoan; Humans; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Restriction Mapping; Tetrahydrofolate Dehydrogenase; Triazines

1995
In vitro susceptibility of Cambodian isolates of Plasmodium falciparum to halofantrine, pyronaridine and artemisinin derivatives.
    Annals of tropical medicine and parasitology, 1994, Volume: 88, Issue:2

    Topics: Adult; Animals; Antimalarials; Artemisinins; Chloroquine; Drug Resistance; Humans; In Vitro Techniques; Mefloquine; Naphthyridines; Phenanthrenes; Plasmodium falciparum; Proguanil; Pyrimethamine; Quinine; Sesquiterpenes; Triazines

1994
In vitro activity of pyrimethamine, cycloguanil, and other antimalarial drugs against African isolates and clones of Plasmodium falciparum.
    The American journal of tropical medicine and hygiene, 1994, Volume: 50, Issue:2

    Topics: Africa; Animals; Antimalarials; Chloroquine; Drug Resistance; Humans; Mefloquine; Phenanthrenes; Plasmodium falciparum; Proguanil; Pyrimethamine; Quinine; Triazines

1994
Plasmodium falciparum: molecular characterization of multidrug-resistant Cambodian isolates.
    Experimental parasitology, 1996, Volume: 82, Issue:2

    Topics: Alleles; Animals; Antimalarials; Blotting, Southern; Cambodia; Chloroquine; Codon; DNA Fingerprinting; DNA, Protozoan; Drug Resistance, Multiple; Folic Acid Antagonists; Genes, Protozoan; Genetic Variation; Humans; Mefloquine; Phenanthrenes; Plasmodium falciparum; Polymorphism, Genetic; Proguanil; Pyrimethamine; Triazines

1996
Point mutations in the dihydrofolate reductase and dihydropteroate synthetase genes and in vitro susceptibility to pyrimethamine and cycloguanil of Plasmodium falciparum isolates from Papua New Guinea.
    The American journal of tropical medicine and hygiene, 1996, Volume: 55, Issue:2

    Topics: Animals; Antimalarials; Base Sequence; Dihydropteroate Synthase; DNA Primers; Drug Resistance; Folic Acid Antagonists; Humans; Malaria, Falciparum; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Triazines

1996
In vitro selection of Plasmodium falciparum lines resistant to dihydrofolate-reductase inhibitors and cross resistance studies.
    Japanese journal of medical science & biology, 1996, Volume: 49, Issue:1

    Topics: Animals; Clone Cells; Drug Resistance; Folic Acid Antagonists; Humans; Methotrexate; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1996
Plasmodium falciparum: mutation pattern in the dihydrofolate reductase-thymidylate synthase genes of Vietnamese isolates, a novel mutation, and coexistence of two clones in a Thai patient.
    Experimental parasitology, 1996, Volume: 84, Issue:1

    Topics: Animals; Antimalarials; Base Sequence; DNA, Protozoan; Drug Resistance; Folic Acid Antagonists; Humans; Malaria, Falciparum; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Thailand; Thymidylate Synthase; Triazines; Vietnam

1996
Susceptibility studies of Plasmodium falciparum isolates and clones against cycloguanil and pyrimethamine using the modified in vitro microtechnique.
    The Journal of parasitology, 1996, Volume: 82, Issue:6

    Topics: Animals; Antimalarials; Clone Cells; Drug Resistance; Folic Acid Antagonists; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

1996
Antifolate-resistant mutants of Plasmodium falciparum dihydrofolate reductase.
    Proceedings of the National Academy of Sciences of the United States of America, 1997, Feb-18, Volume: 94, Issue:4

    Topics: Animals; Antimalarials; Biological Evolution; Drug Resistance; Folic Acid Antagonists; Models, Genetic; Mutagenesis, Site-Directed; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

1997
Effects of folic and folinic acids in the activities of cycloguanil and WR99210 against Plasmodium falciparum in erythrocytic culture.
    Annals of tropical medicine and parasitology, 1997, Volume: 91, Issue:1

    Topics: Animals; Antimalarials; Atovaquone; Drug Interactions; Folic Acid; Humans; Leucovorin; Naphthoquinones; Plasmodium falciparum; Proguanil; Purine Nucleotides; Pyrimethamine; Pyrimidine Nucleotides; Triazines

1997
In vitro sensitivity of Plasmodium falciparum to anti-folinic agents (trimethoprim, pyrimethamine, cycloguanil): a study of 29 African strains.
    Bulletin de la Societe de pathologie exotique (1990), 1997, Volume: 90, Issue:2

    Topics: Animals; Antimalarials; Confidence Intervals; Drug Resistance; Folic Acid Antagonists; Humans; Lethal Dose 50; Malaria, Falciparum; Nonlinear Dynamics; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim

1997
Plasmodium falciparum: asparagine mutant at residue 108 of dihydrofolate reductase is an optimal antifolate-resistant single mutant.
    Experimental parasitology, 1997, Volume: 87, Issue:3

    Topics: Animals; Asparagine; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Genes, Synthetic; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Triazines

1997
Kenyan Plasmodium falciparum field isolates: correlation between pyrimethamine and chlorcycloguanil activity in vitro and point mutations in the dihydrofolate reductase domain.
    Antimicrobial agents and chemotherapy, 1998, Volume: 42, Issue:1

    Topics: Animals; Antimalarials; Humans; Kenya; Malaria, Falciparum; Plasmodium falciparum; Point Mutation; Proguanil; Protozoan Proteins; Pyrimethamine; Sensitivity and Specificity; Tetrahydrofolate Dehydrogenase; Triazines

1998
A biochemical and genetic model for parasite resistance to antifolates. Toxoplasma gondii provides insights into pyrimethamine and cycloguanil resistance in Plasmodium falciparum.
    The Journal of biological chemistry, 1998, Feb-06, Volume: 273, Issue:6

    Topics: Alleles; Animals; Binding Sites; Drug Resistance; Escherichia coli; Folic Acid; Folic Acid Antagonists; Genetic Complementation Test; Kinetics; Models, Genetic; Models, Molecular; Mutagenesis, Site-Directed; NAD; Plasmodium falciparum; Proguanil; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Toxoplasma; Triazines

1998
Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples.
    The American journal of tropical medicine and hygiene, 1999, Volume: 61, Issue:1

    Topics: Alleles; Animals; Antimalarials; DNA Primers; DNA Restriction Enzymes; DNA, Protozoan; Humans; Inhibitory Concentration 50; Kenya; Malaria, Falciparum; Plasmodium falciparum; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines

1999
Gametocytocidal activity of pyronaridine and DNA topoisomerase II inhibitors against multidrug-resistant Plasmodium falciparum in vitro.
    Parasitology international, 2000, Volume: 48, Issue:4

    Topics: Amsacrine; Animals; Antimalarials; Chloroquine; Drug Resistance, Multiple; Enzyme Inhibitors; Etoposide; Humans; Inhibitory Concentration 50; Malaria, Falciparum; Mefloquine; Naphthyridines; Norfloxacin; Nucleic Acid Synthesis Inhibitors; Plasmodium falciparum; Primaquine; Proguanil; Pyrimethamine; Thailand; Topoisomerase II Inhibitors; Triazines

2000
Antibiotics for prophylaxis of Plasmodium falciparum infections: in vitro activity of doxycycline against Senegalese isolates.
    The American journal of tropical medicine and hygiene, 2000, Volume: 62, Issue:1

    Topics: Amodiaquine; Animals; Anti-Bacterial Agents; Antibiotic Prophylaxis; Antimalarials; Artemether; Artemisinins; Chloroquine; Doxycycline; Drug Resistance; Erythrocytes; Humans; Inhibitory Concentration 50; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Pyrimethamine; Quinine; Scintillation Counting; Senegal; Sesquiterpenes; Statistics, Nonparametric; Triazines

2000
Molecular epidemiology of malaria in Yaounde, Cameroon. VI. Sequence variations in the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene and in vitro resistance to pyrimethamine and cycloguanil.
    The American journal of tropical medicine and hygiene, 2000, Volume: 62, Issue:2

    Topics: Animals; Antimalarials; Cameroon; DNA Primers; DNA, Protozoan; Drug Resistance; Folic Acid Antagonists; Humans; Inhibitory Concentration 50; Malaria, Falciparum; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Triazines

2000
Interaction of pyrimethamine, cycloguanil, WR99210 and their analogues with Plasmodium falciparum dihydrofolate reductase: structural basis of antifolate resistance.
    Bioorganic & medicinal chemistry, 2000, Volume: 8, Issue:5

    Topics: Amino Acid Sequence; Drug Resistance; Folic Acid Antagonists; Models, Molecular; Molecular Sequence Data; Molecular Structure; Proguanil; Pyrimethamine; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2000
Genome comparison of progressively drug resistant Plasmodium falciparum lines derived from drug sensitive clone.
    Memorias do Instituto Oswaldo Cruz, 2001, Volume: 96, Issue:3

    Topics: Animals; Antimalarials; DNA, Protozoan; Drug Resistance; Genome, Protozoan; Humans; Parasitic Sensitivity Tests; Plasmodium falciparum; Polymorphism, Restriction Fragment Length; Proguanil; Pyrimethamine; Sulfadoxine; Time Factors; Triazines

2001
Homology modeling of wild type and pyrimethamine/cycloguanil-cross resistant mutant type Plasmodium falciparum dihydrofolate reductase. A model for antimalarial chemotherapy resistance.
    Biophysical chemistry, 2001, Jul-24, Volume: 91, Issue:3

    Topics: Amino Acid Sequence; Animals; Antimalarials; Binding Sites; Chickens; Drug Resistance; Folic Acid Antagonists; Humans; Liver; Malaria; Models, Biological; Models, Molecular; Molecular Sequence Data; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2001
Novel alleles of the Plasmodium falciparum dhfr highly resistant to pyrimethamine and chlorcycloguanil, but not WR99210.
    Molecular and biochemical parasitology, 2001, Sep-28, Volume: 117, Issue:1

    Topics: Alleles; Amino Acid Substitution; Animals; Antimalarials; Drug Resistance; Genes, Protozoan; Inhibitory Concentration 50; Models, Molecular; Molecular Sequence Data; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Protein Conformation; Pyrimethamine; Saccharomyces cerevisiae; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Triazines

2001
Molecular modeling of wild-type and antifolate resistant mutant Plasmodium falciparum DHFR.
    Biophysical chemistry, 2002, Aug-02, Volume: 98, Issue:3

    Topics: Animals; Chickens; Drug Resistance; Folic Acid Antagonists; Humans; Liver; Malaria, Falciparum; Models, Chemical; Models, Genetic; Models, Molecular; Molecular Sequence Data; Plasmodium falciparum; Point Mutation; Proguanil; Pyrimethamine; Sequence Alignment; Tetrahydrofolate Dehydrogenase; Triazines

2002
Pyrimethamine and WR99210 exert opposing selection on dihydrofolate reductase from Plasmodium vivax.
    Proceedings of the National Academy of Sciences of the United States of America, 2002, Oct-01, Volume: 99, Issue:20

    Topics: Alleles; Amino Acid Sequence; Animals; Antimalarials; Dose-Response Relationship, Drug; Drug Resistance; Inhibitory Concentration 50; Malaria; Molecular Sequence Data; Mutagenesis, Site-Directed; Mutation; Plasmids; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Recombinant Proteins; Sequence Homology, Amino Acid; Tetrahydrofolate Dehydrogenase; Triazines

2002
[Gene point mutation in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum].
    Zhongguo ji sheng chong xue yu ji sheng chong bing za zhi = Chinese journal of parasitology & parasitic diseases, 2001, Volume: 19, Issue:2

    Topics: Animals; Drug Resistance; Multienzyme Complexes; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Polymorphism, Restriction Fragment Length; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

2001
In vitro sensitivity of Plasmodium falciparum to amodiaquine compared with other major antimalarials in Madagascar.
    Parassitologia, 2002, Volume: 44, Issue:3-4

    Topics: Amodiaquine; Animals; Antimalarials; Chloroquine; Drug Resistance; Drug Resistance, Multiple; Humans; Inhibitory Concentration 50; Madagascar; Malaria, Falciparum; Mefloquine; Parasitemia; Plasmodium falciparum; Proguanil; Pyrimethamine; Quinine; Triazines

2002
Novel point mutations in the dihydrofolate reductase gene of Plasmodium vivax: evidence for sequential selection by drug pressure.
    Antimicrobial agents and chemotherapy, 2003, Volume: 47, Issue:5

    Topics: Animals; Drug Resistance; Folic Acid Antagonists; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2003
DHFR and DHPS genotypes of Plasmodium falciparum isolates from Gabon correlate with in vitro activity of pyrimethamine and cycloguanil, but not with sulfadoxine-pyrimethamine treatment efficacy.
    The Journal of antimicrobial chemotherapy, 2003, Volume: 52, Issue:1

    Topics: Animals; Antimalarials; Dihydropteroate Synthase; DNA, Protozoan; Gabon; Genotype; Humans; Plasmodium falciparum; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines

2003
Short communication: Prevalence of mutations associated with resistance to atovaquone and to the antifolate effect of proguanil in Plasmodium falciparum isolates from northern Ghana.
    Tropical medicine & international health : TM & IH, 2004, Volume: 9, Issue:3

    Topics: Animals; Antimalarials; Atovaquone; Child, Preschool; Cytochromes b; Drug Combinations; Drug Resistance; Drug Synergism; Drug Therapy, Combination; Female; Folic Acid Antagonists; Ghana; Humans; Infant; Malaria, Falciparum; Male; Mutation; Naphthoquinones; Plasmodium falciparum; Polymorphism, Restriction Fragment Length; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines

2004
Novel alleles of Plasmodium falciparum dhfr that confer resistance to chlorcycloguanil.
    Molecular and biochemical parasitology, 2005, Volume: 139, Issue:1

    Topics: Alleles; Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Mutagenesis, Site-Directed; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2005
Stoichiometric selection of tight-binding inhibitors by wild-type and mutant forms of malarial (Plasmodium falciparum) dihydrofolate reductase.
    Analytical chemistry, 2005, Mar-01, Volume: 77, Issue:5

    Topics: Algorithms; Animals; Chromatography, High Pressure Liquid; Combinatorial Chemistry Techniques; Folic Acid Antagonists; Humans; Kinetics; Mass Spectrometry; Molecular Structure; Mutation; Plasmodium falciparum; Proguanil; Protein Binding; Pyrimethamine; Recombinant Proteins; Reproducibility of Results; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim

2005
A simple dual selection for functionally active mutants of Plasmodium falciparum dihydrofolate reductase with improved solubility.
    Protein engineering, design & selection : PEDS, 2005, Volume: 18, Issue:10

    Topics: Amino Acid Sequence; Animals; Cloning, Molecular; Folic Acid Antagonists; Gene Library; Genes, Reporter; Genetic Complementation Test; Green Fluorescent Proteins; Hydrophobic and Hydrophilic Interactions; Kinetics; Mutagenesis, Site-Directed; Mutation; Plasmodium falciparum; Proguanil; Protein Engineering; Protein Structure, Quaternary; Pyrimethamine; Recombinant Fusion Proteins; Solubility; Tetrahydrofolate Dehydrogenase; Triazines

2005
Plasmodium falciparum: interaction of shikimate analogues with antimalarial drugs.
    Experimental parasitology, 2005, Volume: 111, Issue:3

    Topics: Animals; Antimalarials; Atovaquone; Drug Interactions; Naphthoquinones; Plasmodium falciparum; Proguanil; Pyrimethamine; Shikimic Acid; Triazines

2005
Susceptibility studies of Malaysian Plasmodium falciparum clones to type II antifolate drugs after 3 years of continuous in vitro culture.
    Chemotherapy, 2005, Volume: 51, Issue:6

    Topics: Animals; Antimalarials; Clone Cells; Drug Resistance; Folic Acid Antagonists; In Vitro Techniques; Malaysia; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

2005
Amino acid mutations in Plasmodium vivax DHFR and DHPS from several geographical regions and susceptibility to antifolate drugs.
    The American journal of tropical medicine and hygiene, 2006, Volume: 75, Issue:4

    Topics: Amino Acid Sequence; Animals; Antimalarials; Asia, Southeastern; China; Dihydropteroate Synthase; Drug Combinations; Drug Resistance; Folic Acid Antagonists; Humans; Melanesia; Molecular Sequence Data; Plasmodium vivax; Point Mutation; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines

2006
The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase.
    International journal for parasitology, 2007, Volume: 37, Issue:7

    Topics: Animals; Catalysis; DNA, Protozoan; Enzyme Stability; Escherichia coli; Folic Acid Antagonists; Genetic Complementation Test; Kinetics; Mutagenesis, Insertional; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Tryptophan

2007
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
    Antimicrobial agents and chemotherapy, 2007, Volume: 51, Issue:12

    Topics: Animals; Antimalarials; Drug Resistance; Drug Resistance, Multiple; Kinetics; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2007
Effect of folate derivatives on the activity of antifolate drugs used against malaria and cancer.
    Parasitology research, 2008, Volume: 102, Issue:6

    Topics: Aminopterin; Animals; Antimalarials; Antineoplastic Agents; Folic Acid; Folic Acid Antagonists; Inhibitory Concentration 50; Leucovorin; Methotrexate; Molecular Structure; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolates; Triazines; Trimetrexate

2008
Escalating Plasmodium falciparum antifolate drug resistance mutations in Macha, rural Zambia.
    Malaria journal, 2008, May-21, Volume: 7

    Topics: Animals; Antimalarials; Child; Child, Preschool; DNA, Protozoan; Drug Resistance; Folic Acid Antagonists; Humans; Malaria, Falciparum; Mutation, Missense; Peptide Synthases; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Polymorphism, Restriction Fragment Length; Proguanil; Protozoan Proteins; Pyrimethamine; Rural Population; Tetrahydrofolate Dehydrogenase; Triazines; Zambia

2008
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.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:9

    Topics: Animals; Antimalarials; Folic Acid Antagonists; Genotype; Inhibitory Concentration 50; Kenya; Methotrexate; Mutation; Plasmodium falciparum; Polymerase Chain Reaction; Polymorphism, Genetic; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim; Trimetrexate

2009
Shape- and chemical feature-based 3D-pharmacophore model generation and virtual screening: identification of potential leads for P. falciparum DHFR enzyme inhibition.
    Chemical biology & drug design, 2010, Volume: 75, Issue:1

    Topics: Amino Acid Sequence; Animals; Antimalarials; DNA, Protozoan; Folic Acid Antagonists; Humans; Molecular Sequence Data; Plasmodium falciparum; Proguanil; Protein Binding; Pyrimethamine; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines; X-Rays

2010
Fitness trade-offs in the evolution of dihydrofolate reductase and drug resistance in Plasmodium falciparum.
    PloS one, 2011, Volume: 6, Issue:5

    Topics: Drug Resistance; Evolution, Molecular; Folic Acid Antagonists; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines

2011
Cloning and heterologous expression of Plasmodium ovale dihydrofolate reductase-thymidylate synthase gene.
    Parasitology international, 2012, Volume: 61, Issue:2

    Topics: Amino Acid Sequence; Antimalarials; Cloning, Molecular; Escherichia coli; Folic Acid Antagonists; Genetic Complementation Test; Hydrogen-Ion Concentration; Kinetics; Molecular Sequence Data; Multienzyme Complexes; Plasmodium ovale; Proguanil; Protozoan Proteins; Pyrimethamine; Sequence Alignment; Sequence Analysis, DNA; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

2012
Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.
    PloS one, 2012, Volume: 7, Issue:7

    Topics: Amino Acid Substitution; Antimalarials; Cells, Cultured; Drug Resistance; Erythrocytes; Folic Acid Antagonists; Gene Dosage; Humans; Inhibitory Concentration 50; Mutagenesis, Insertional; Plasmodium falciparum; Plasmodium vivax; Proguanil; Protozoan Proteins; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Transfection; Triazines

2012
Mycobacterium tuberculosis dihydrofolate reductase reveals two conformational states and a possible low affinity mechanism to antifolate drugs.
    Structure (London, England : 1993), 2014, Jan-07, Volume: 22, Issue:1

    Topics: Bacterial Proteins; Calorimetry; Crystallography, X-Ray; Enzyme Inhibitors; Escherichia coli; Folic Acid Antagonists; Ligands; Molecular Docking Simulation; Mutagenesis, Site-Directed; Mycobacterium tuberculosis; Proguanil; Protein Conformation; Pyrimethamine; Recombinant Proteins; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Thermodynamics; Triazines; Trimethoprim

2014
Adaptive Landscape by Environment Interactions Dictate Evolutionary Dynamics in Models of Drug Resistance.
    PLoS computational biology, 2016, Volume: 12, Issue:1

    Topics: Antimalarials; Computational Biology; Drug Resistance; Evolution, Molecular; Humans; Inhibitory Concentration 50; Malaria, Falciparum; Models, Biological; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines

2016
Herbicidal properties of antimalarial drugs.
    Scientific reports, 2017, 03-31, Volume: 7

    Topics: Antimalarials; Arabidopsis; Herbicides; Humans; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Pyrimethamine; Sulfadiazine; Sulfadoxine; Triazines

2017
Comparison of the susceptibility of Plasmodium knowlesi and Plasmodium falciparum to antimalarial agents.
    The Journal of antimicrobial chemotherapy, 2017, Nov-01, Volume: 72, Issue:11

    Topics: Antimalarials; Benzothiazoles; Colorimetry; Diamines; Dihydroorotate Dehydrogenase; Erythrocytes; Fluorescence; Humans; L-Lactate Dehydrogenase; Malaria; Organic Chemicals; Oxidoreductases Acting on CH-CH Group Donors; Parasitic Sensitivity Tests; Plasmodium falciparum; Plasmodium knowlesi; Proguanil; Pyrimethamine; Quinolines; Sensitivity and Specificity; Triazines

2017
Characterization of Plasmodium knowlesi dihydrofolate reductase-thymidylate synthase and sensitivity to antifolates.
    Parasitology international, 2018, Volume: 67, Issue:6

    Topics: Antimalarials; Base Sequence; Folic Acid Antagonists; Multienzyme Complexes; Plasmodium knowlesi; Proguanil; Protozoan Proteins; Pyrimethamine; Sequence Alignment; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines

2018
Discovery of new non-pyrimidine scaffolds as
    Journal of enzyme inhibition and medicinal chemistry, 2021, Volume: 36, Issue:1

    Topics: Antimalarials; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Enzyme Inhibitors; Models, Molecular; Molecular Docking Simulation; Molecular Structure; Plasmodium falciparum; Proguanil; Protozoan Proteins; Pyrimethamine; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines

2021