cycloguanil has been researched along with proguanil in 185 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 35 (18.92) | 18.7374 |
| 1990's | 64 (34.59) | 18.2507 |
| 2000's | 56 (30.27) | 29.6817 |
| 2010's | 28 (15.14) | 24.3611 |
| 2020's | 2 (1.08) | 2.80 |
| Authors | Studies |
|---|---|
| Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; O'Neil, MT; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, PL; Yang, YS | 1 |
| García-Mera, X; González-Díaz, H; Prado-Prado, FJ | 1 |
| Cichero, E; Espinoza, S; Gainetdinov, RR; Tonelli, M | 1 |
| Cichero, E; Costi, MP; Gazzarrini, S; Loddo, R; Moroni, A; Naesens, L; Santucci, M; Tasso, B; Tonelli, M | 1 |
| Bosco, O; Funck-Brentano, C; Jacqz-Aigrain, E; Jaillon, P; Keundjian, A | 1 |
| Gyang, FN; Peterson, DS; Wellems, TE | 1 |
| Breckenridge, AM; Brøsen, K; Gram, LF; Helsby, NA; Skjelbo, E; Ward, SA | 1 |
| González-Ruiz, A; Haworth, SJ; O'Neil, AB; Warhurst, DC | 1 |
| Björkman, A; Flachs, H; Hanson, AP; Hvidberg, EF; Høgh, B; Petersen, E | 1 |
| Bjorkman, A; Flacks, H; Hanson, AP; Hogh, B; Petersen, E | 1 |
| Cowman, AF; Foote, SJ; Galatis, D | 1 |
| Milhous, WK; Peterson, DS; Wellems, TE | 1 |
| Edstein, MD; Rieckmann, KH; Veenendaal, JR | 2 |
| Jamaludin, A; Mohamad, M; Navaratnam, V; Wernsdorfer, WH; Yeoh, PY | 1 |
| Breckenridge, AM; Edwards, G; Helsby, NA; Howells, RE; Ward, SA | 1 |
| Koetzle, TF; Schwalbe, CH; Williams, GJ | 1 |
| Breckenridge, AM; Gilles, HM; Howells, RE; Koech, DK; Mberu, E; Saunders, JE; Ward, SA; Watkins, WM | 1 |
| Berlin, OG; Bruckner, DA; Gonzalez, AH | 1 |
| Chiluba, EM; Fletcher, KA; Price, AH | 1 |
| Edstein, MD; Rieckmann, KH; Scott, HV; Veenendaal, JR | 2 |
| Gajanana, A; Ramanaiah, TV | 1 |
| Flachs, H; Hanson, AP; Høgh, B; Petersen, E | 1 |
| Booth, RG; Hansch, C; Neal, RA; Santi, DV; Sertsrivanich, R; Sirawaraporn, W | 1 |
| Barutwanayo, M; Coosemans, MH; Gryseels, B; Onori, E; Otoul, C; Wéry, M | 1 |
| O'Sullivan, WJ; Rieckmann, KH; Scott, HV | 1 |
| Looareesuwan, S; Moody, RR; Ochekpe, NA; Taylor, RB; Wattanagoon, Y; White, NJ | 1 |
| Edstein, MD; Veenendaal, JR | 1 |
| Childs, GE; Lambros, C | 1 |
| Koech, DK; Sixsmith, DG; Spencer, HC; Watkins, WW | 1 |
| Howells, RE; Percy, M | 1 |
| Moody, RR; Ochekpe, NA; Taylor, RB | 1 |
| Bygbjerg, I; Flachs, H; Hvidberg, EF; Ravn, P; Rønn, A | 1 |
| Bygbjerg, IC; Flachs, H | 1 |
| Edstein, MD | 1 |
| Fletcher, KA; Kelly, JA | 1 |
| Bygbjerg, IC | 1 |
| Barber, AM; Campbell, CC; Collins, WE; Nguyen-Dinh, P; Teklehaimanot, A | 1 |
| Greenwood, BM; Panton, LJ | 1 |
| Bent, NS; Gilles, HM; Howells, RE | 1 |
| Schapira, A | 1 |
| Chulay, JD; Sixsmith, DG; Spencer, HC; Watkins, WM | 1 |
| Chulay, JD; Sixsmith, DG; Watkins, WM | 1 |
| Rossan, RN; Schmidt, LH | 1 |
| Høiby, N; Kharazmi, A; Valerius, NH | 1 |
| Bird, K; Hunt, WE; Mallinson, PD; Schwalbe, CH | 1 |
| Howells, RE; Judge, BM | 1 |
| Graham, NB; Howells, RE; Judge, BM; McNeill, ME | 1 |
| Moody, RR; Selkirk, AB; Taylor, RB | 1 |
| Funck-Brentano, C; Jacqz-Aigrain, E; Jaillon, P; Keundjian, A; Partovian, C | 1 |
| Chiba, K; Darmansjah, I; Ishizaki, T; Kusaka, M; Setiabudy, R | 1 |
| Basco, LK; Eldin de Pécoulas, P; Le Bras, J; Mazabraud, A; Wilson, CM | 1 |
| Abdallah, B; Basco, LK; Djé, MK; Eldin de Pécoulas, P; Le Bras, J; Mazabraud, A | 1 |
| Edstein, MD; Rieckmann, KH; Shanks, GD; Yeo, AE | 2 |
| Andersson, T; Birkett, DJ; Gonzalez, FJ; Miners, JO; Rees, D; Veronese, ME | 1 |
| Basco, LK; Le Bras, J | 2 |
| Holfels, E; Mack, D; McAuley, J; McLeod, R; Milhous, WK | 1 |
| Basco, LK; Le Bras, J; Ramiliarisoa, O | 1 |
| Edstein, MD; Rieckmann, KH; Shanks, GD; Teja-Isavadharm, P; Webster, HK | 1 |
| Breckenridge, AM; Edwards, G; Helsby, NA; Ward, SA | 1 |
| Ager, AL; Canfield, CJ; Jacobus, DP; Lewis, NJ; Milhous, WK; Rossan, RN; Sweeney, TR | 1 |
| Brøsen, K; Flachs, H; Skjelbo, E | 1 |
| Moody, RR; Nosten, F; Taylor, RB; ter Kuile, F; Wangboonskul, J; White, NJ | 1 |
| Basco, LK; Doury, JC; Le Bras, J; Ramiliarisoa, O; Ringwald, P | 1 |
| Doury, JC; Fusai, T; Keundjian, A; Touze, JE | 1 |
| Basco, LK; de Pecoulas, PE; Le Bras, J; Wilson, CM | 1 |
| Chiba, K; Ishizaki, T; Kusaka, M; Setiabudy, R | 1 |
| Kolawole, JA; Moody, RR; Taylor, RB | 1 |
| Cowman, AF; Genton, B; Lorry, K; Reeder, JC; Rieckmann, KH; Wines, B | 1 |
| Bhasin, VK; Nair, L | 1 |
| Alexander, C; Nathwani, D; Taylor, RB; Zimbler, N | 1 |
| Bochner, F; Reinhard, HA; Somogyi, AA | 1 |
| Nguyen, DS; Nguyen, PD; Sköld, O; Swedberg, G; Zindrou, S | 1 |
| Ang, HH; Chan, KL; Mak, JW | 1 |
| Beaune, P; Becquemont, L; Funck-Brentano, C; Jaillon, P; Lenevu, A; Roux, A | 1 |
| Santi, DV; Sathitkul, T; Sirawaraporn, R; Sirawaraporn, W; Yuthavong, Y | 1 |
| Christopherson, RI; Rieckmann, KH; Seymour, KK; Yeo, AE | 1 |
| Bahr, S; Edstein, MD; Kotecka, B; Rieckmann, KH; Shanks, GD | 1 |
| Brøsen, K; Jeppesen, U; Rasmussen, BB | 1 |
| Santi, DV; Sirawaraporn, R; Sirawaraporn, W; Yongkiettrakul, S; Yuthavong, Y | 1 |
| Doerig, C; Doury, JC; Fusai, T; Parzy, D; Pradines, B; Rico, A | 1 |
| Mberu, EK; Nzila-Mounda, A; Plowe, CV; Sibley, CH; Watkins, WM; Winstanley, PA | 1 |
| Reynolds, MG; Roos, DS | 1 |
| Friedmann, PS; Helsby, NA; Parslew, RA; Rhodes, LE; Ward, SA | 1 |
| Bergqvist, Y; Funding, L; Krysèn, B; Leek, T; Yvell, K | 1 |
| Christopherson, RI; Yeo, AE | 1 |
| di Piazza, JP; Durand, R; Le Bras, J; Longuet, C; Parzy, D; Pradines, B | 1 |
| Gross, AS; Hoskins, JM; Shenfield, GM | 2 |
| Fidock, DA; Nomura, T; Wellems, TE | 1 |
| Bergqvist, Y; Funding, L; Kaneko, A; Krysén, B; Leek, T | 1 |
| Bergqvist, Y; Björkman, A; Ishizaki, T; Kalkoa, M; Kaneko, A; Kaneko, O; Kobayakawa, T; Takechi, M | 1 |
| Bouchaud, O; di Piazza, JP; Durand, R; Godineau, N; Le Bras, J; Longuet, C; Marchou, B; Martet, G; Parzy, D; Pradines, B; Roué, R | 1 |
| Fusai, T; Keundjian, A; Kombila, M; Lebeau, C; Mabika Mamfoumbi, M; Owono Medang, M; Parzy, D; Pradines, B; Rogier, C | 1 |
| Bochner, F; Coller, JK; Somogyi, AA | 1 |
| Gillotin, C; Mamet, JP; Veronese, L | 1 |
| Howard, V; Mookherjee, S; Nzila-Mouanda, A; Sibley, CH; Watkins, W | 1 |
| Clain, J; di Piazza, JP; Durand, R; le Bras, J; Longuet, C; Sécardin, Y | 1 |
| Bathum, L; Brøsen, K; Hørder, M; Madsen, H; Mutabingwa, TK; Skjelbo, E | 1 |
| Basco, LK; Ndounga, M; Ringwald, P | 1 |
| Abdul-Aguye, I; Kolawole, JA; Mustapha, A; Ochekpe, N; Taylor, RB | 1 |
| Auparakkitanon, S; Chavalitshewinkoon-Petmitr, P; Pongvilairat, G; Wilairat, P | 1 |
| Fusai, T; Mosnier, J; Parzy, D; Pradines, B; Rogier, C; Spiegel, A; Tall, A; Trape, JF | 1 |
| Basco, LK; Ringwald, P | 1 |
| Kamchonwongpaisan, S; Lowe, G; Quarrell, R; Rastelli, G; Sirawaraporn, W; Sompornpisut, P; Thebtaranonth, Y; Vilaivan, T; Yuthavong, Y | 1 |
| Chareonsethakul, N; Kamchonwongpaisan, S; Lowe, G; Quarrell, R; Sirawaraporn, W; Vilaivan, T; Yuthavong, Y | 1 |
| Alm, C; Bertilsson, L; Ericsson, O; Gustafsson, LL; Herrlin, K; Massele, AY; Rais, M; Rimoy, G | 1 |
| Bhasin, V; Nair, L; Toteja, R | 1 |
| Low, AS; Reid, RG; Taylor, RB | 1 |
| Huang, SL; Lu, AH; Ou-Yang, DS; Shu, Y; Wang, W; Zhou, HH | 1 |
| de Alencastro, RB; Figueroa-Villar, JD; Santos-Filho, OA | 1 |
| Hankins, EG; Sibley, CH; Warhurst, DC | 1 |
| Ashton, M; Bergqvist, Y; Björkman, A; Johansson, I; Lindegårdh, N; Nivelius, S; Thapar, MM | 1 |
| Delfino, RT; Figueroa-Villar, JD; Santos-Filho, OA | 1 |
| Hastings, MD; Sibley, CH | 1 |
| Jarprung, D; Kamchonwongpaisan, S; Saesaengseerung, N; Sirawaraporn, W; Vilaivan, T; Yuthavong, Y | 1 |
| Liu, H; Yang, YM; Zhang, ZX | 1 |
| Bouchaud, O; Durand, R; Godineau, N; Jezic, Z; Keundjian, A; Le Bras, J; Pradines, B; Ralaimazava, P | 1 |
| Alifrangis, M; Jelinek, T; Salanti, A; Schwöbel, B | 1 |
| Durand, R; Le Bras, J | 1 |
| Ariey, F; Duchemin, JB; Harisoa, JL; Mauclere, P; Pietra, V; Rabarijaona, LP; Raharimalala, LA; Rakotomanana, F; Ranaivo, L; Randrianarivelojosia, M; Robert, V | 1 |
| Charlieu, JP; Imwong, M; Leartsakulpanich, U; Letourneur, F; Looareesuwan, S; Pukrittayakamee, S; Rénia, L; Snounou, G; White, NJ | 1 |
| Aubouy, A; Bakary, M; Deloron, P; Durand, R; Huart, V; Jafari, S; Le Bras, J; Mayombo, J; Migot-Nabias, F | 1 |
| Ashley, E; Cho, D; Cho, T; Edstein, MD; Ginsberg, A; Looareesuwan, S; McGready, R; Nosten, F; Seaton, E; Stepniewska, K; White, NJ | 1 |
| Charoensetakul, N; Kamchonwongpaisan, S; Lowe, G; Ponsinet, R; Quarrell, R; Sirawaraporn, W; Tarnchompoo, B; Vanichtanankul, J; Vilaivan, T; Yuthavong, Y | 1 |
| Rakotoson, JD; Randremanana, RV; Randriamanantena, A; Randrianarivelojosia, M; Randrianasolo, L; Ratsimbasoa, A | 1 |
| Bienzle, U; Ehrhardt, S; Jelinek, T; Mockenhaupt, FP; Muehlen, M; Otchwemah, R; Schreiber, J | 1 |
| Björkman, A; Gil, JP; Thapar, MM | 1 |
| Hunt, SY; Rezvani, BB; Sibley, CH | 1 |
| Agarwal, A; Chauhan, PM; Puri, SK; Srivastava, K | 1 |
| Peters, W; Robinson, BL; Stewart, LB | 1 |
| Kamchonwongpaisan, S; Tarnchompoo, B; Taweechai, S; Vanichtanankul, J; Yuthavong, Y; Yuvaniyama, J | 1 |
| Kioy, D; Konsil, J; Manyando, C; Miller, GB; Mulenga, M; Na-Bangchang, K; Ruengweerayut, R | 1 |
| Chusacultanachai, S; Japrung, D; Wilairat, P; Yuthavong, Y; Yuvaniyama, J | 1 |
| Hunt, S; Kamau, EM; Nduati, E; Nzila, A | 1 |
| Jiang, S; McConkey, GA; McRobert, L; Stead, A | 1 |
| Ang, HH; Cheang, HS; Mak, JW | 1 |
| Charman, WN; Chiu, FC; Leveque, NL | 1 |
| Kamau, EM; Nduati, EW | 1 |
| Aarons, L; Bojang, K; Edwards, G; Hughes, D; Manyando, C; Simpson, JA; Ward, S; Watkins, WA; Winstanley, P | 1 |
| Anh, le N; Auliff, A; Bell, D; Chen, N; Cheng, Q; Gao, Q; Maguire, J; O'Neil, MT; Russell, B; Wilson, DW | 1 |
| Gourmel, B; Houzé, P; Houzé, S; Le bras, J; Le bricon, T; Lejeune, D; Souletie, I | 1 |
| Chitnumsub, P; Kamchonwongpaisan, S; Taweechai, S; Vanichtanankul, J; Yuthavong, Y | 1 |
| Adithan, C; Rajan, S; Shashindran, C; Tushar, T; Vinod, T | 1 |
| Chusacultanachai, S; Japrung, D; Leartsakulpanich, U; Yuthavong, Y | 1 |
| Asher, CO; Diaz, DS; Jacobus, DP; Kozar, MP; Milhous, WK; Schiehser, GA; Shearer, TW; Skillman, DR; Smith, KS; Sousa, JC | 1 |
| Diriye, A; Kiara, S; Kokwaro, G; Masseno, V; Mwai, L; Nduati, E; Nzila, A; Ommeh, S | 1 |
| Chishimba, S; Mharakurwa, S; Mkulama, MA; Rouse, P; Sikalima, J; Thuma, PE | 1 |
| Chauhan, PM; Kumar, A; Puri, SK; Raja Kumar, S; Srivastava, K | 1 |
| Hannongbua, S; Kamchonwongpaisan, S; Maitarad, P; Vanichtanankul, J; Vilaivan, T; Yuthavong, Y | 1 |
| Fogel, GB; Hecht, D | 1 |
| Borrmann, S; Kiara, SM; Masseno, V; Mwai, L; Nzila, A; Ochola, I; Okombo, J | 1 |
| Doerksen, RJ; Sivaprakasam, P; Tosso, PN | 1 |
| Chapman, HL; Conway, DJ; Dunyo, S; Hamid-Adiamoh, M; Janha, RE; Miller, AK; Milligan, P; Opara, H; Pirmohamed, M; Rockett, K; Sisay-Joof, F; Walton, RT; Winstanley, P; Worwui, A | 1 |
| Adane, L; Bharatam, PV | 1 |
| Adane, L; Bharatam, PV; Patel, DS | 1 |
| Basak, SC; Mills, D | 1 |
| Ojha, PK; Roy, K | 1 |
| Brown, KM; Costanzo, MS; Hartl, DL | 1 |
| Imwong, M; Kongsaeree, P; Leartsakulpanich, U; Riangrungroj, P; Tirakarn, S; Yuthavong, Y | 1 |
| Chitnumsub, P; Kamchonwongpaisan, S; Taweechai, S; Uttamapinant, C; Vanichtanankul, J; Vilaivan, T; Yuthavong, Y | 1 |
| Adams, JH; Auliff, AM; Balu, B; Chen, N; Cheng, Q; O'Neil, MT | 1 |
| Blundell, TL; Dias, MV; Domingues, RR; Paes Leme, AF; Tyrakis, P | 1 |
| Bridges, HR; Hirst, J; Jones, AJ; Pollak, MN | 1 |
| Abbat, S; Arfeen, M; Bharatam, PV; Patel, DS; Taxak, N | 1 |
| Chua, HH; Cobbold, SA; Creek, DJ; McConville, MJ; Nijagal, B; Ralph, SA | 1 |
| Dinter, D; Domijan, AM; Gajski, G; Garaj-Vrhovac, V | 1 |
| Diakite, I; Hartl, DL; Ogbunugafor, CB; Weinreich, DM; Wylie, CS | 1 |
| Barata, L; Boutbibe, K; Clain, J; Franetich, JF; Houzé, P; Mazier, D; Zanghi, G | 1 |
| Andrews, KT; Arnold, MS; Chua, MJ; Engel, JA; Fisher, GM; Skinner-Adams, TS | 1 |
| Corral, MG; Leroux, J; Mylne, JS; Stubbs, KA | 1 |
| Blasco, B; Moon, RW; Sutherland, CJ; van Schalkwyk, DA | 1 |
| Bilos, A; Hurkmans, EGE; Koenderink, JB; Rijpma, SR; Russel, FGM; Sauerwein, RW; van den Heuvel, JJMW; van der Velden, M | 1 |
| Brockmöller, J; Jensen, O; Matthaei, J; Prukop, T; Seitz, T; Tadjerpisheh, S; Tann, A; Tzvetkov, MV | 1 |
| Ittarat, W; Kongkasuriyachai, D; Leartsakulpanich, U; Leelayoova, S; Mungthin, M; Pornthanakasem, W; Suwandittakul, N; Tarnchompoo, B; Yuthavong, Y | 1 |
| Inthajak, K; Lawtrakul, L; Toochinda, P | 1 |
| Colafrancesco, V; Dugas, JC; Fernandez-Diez, B; Frade, JM; Giralt, E; Lariosa-Willingham, KD; Leonoudakis, D; López-Sánchez, N; Masso, M; Messeguer, A; Messeguer, J; Moreno, B; Pertsovskaya, I; Pulido-Valdeolivas, I; Steinman, L; Teixido, M; Vazquez, R; Vendrell-Navarro, G; Vila, G; Villoslada, P; Zubizarreta, I | 1 |
| Funakoshi, R; Furihata, K; Ito, K; Kudo, T; Kusuhara, H; Tomoda, Y | 1 |
| Bertolacini, CP; Borsari, C; Cordeiro-da-Silva, A; Costi, MP; Gul, S; Kuzikov, M; Landi, G; Linciano, P; Mangani, S; Moraes, CB; Pozzi, C; Witt, G | 1 |
| Andrews, KT; Antonova-Koch, Y; Burrows, JN; Chopra, P; Clarke, M; Fidock, DA; Fisher, GM; Hutt, OE; Jarvis, KE; Meister, S; Riches, AG; Ryan, JH; Skinner-Adams, TS; von Itzstein, M; Wilson, T; Winzeler, EA | 1 |
| Hoarau, M; Kamchonwongpaisan, S; Srimongkolpithak, N; Vanichtanankul, J; Vitsupakorn, D; Yuthavong, Y | 1 |
| Jang, IJ; Ji, SC; Lee, S; Yang, E | 1 |
1 review(s) available for cycloguanil and proguanil
| Article | Year |
|---|---|
The mechanisms of resistance to antimalarial drugs in Plasmodium falciparum.
Topics: Africa; Animals; Antimalarials; Antimetabolites; Chloroquine; Drug Resistance; Drug Resistance, Multiple; Humans; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 2003 |
15 trial(s) available for cycloguanil and proguanil
| Article | Year |
|---|---|
Relation between chloroguanide bioactivation to cycloguanil and the genetically determined metabolism of mephenytoin in humans.
Topics: Adult; Aryl Hydrocarbon Hydroxylases; Biotransformation; Cytochrome P-450 Enzyme System; Dextromethorphan; Female; Humans; Hydroxylation; Male; Mephenytoin; Polymorphism, Genetic; Prodrugs; Proguanil; Steroid 16-alpha-Hydroxylase; Steroid Hydroxylases; Triazines | 1992 |
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.
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 |
Comparison of chloroguanide and mephenytoin for the in vivo assessment of genetically determined CYP2C19 activity in humans.
Topics: Adult; Cross-Over Studies; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Enzyme Inhibitors; Humans; Hydroxylation; Isoenzymes; Male; Mephenytoin; Omeprazole; Proguanil; Triazines | 1995 |
Fluvoxamine inhibits the CYP2C19-catalyzed bioactivation of chloroguanide.
Topics: Administration, Oral; Adult; Antimetabolites; Aryl Hydrocarbon Hydroxylases; Biguanides; Biotransformation; Cross-Over Studies; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Interactions; Fluvoxamine; Folic Acid Antagonists; Humans; Male; Mephenytoin; Mixed Function Oxygenases; Proguanil; Selective Serotonin Reuptake Inhibitors; Triazines | 1997 |
Lack of a pharmacokinetic interaction between atovaquone and proguanil.
Topics: Adult; Antimalarials; Atovaquone; Cross-Over Studies; Drug Interactions; Female; Humans; Male; Naphthoquinones; Proguanil; Sex Factors; Triazines | 1999 |
Effects of cimetidine on the pharmacokinetics of proguanil in healthy subjects and in peptic ulcer patients.
Topics: Adult; Anti-Ulcer Agents; Antimalarials; Area Under Curve; Cimetidine; Drug Interactions; Humans; Male; Peptic Ulcer; Proguanil; Triazines | 1999 |
Slow chloroguanide metabolism in Tanzanians compared with white subjects and Asian subjects confirms a decreased CYP2C19 activity in relation to genotype.
Topics: Antimalarials; Aryl Hydrocarbon Hydroxylases; Asian People; Black People; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Female; Genotype; Humans; Male; Mixed Function Oxygenases; Proguanil; Tanzania; Triazines; White People | 2000 |
Time-dependent pharmacokinetics and drug metabolism of atovaquone plus proguanil (Malarone) when taken as chemoprophylaxis.
Topics: Adult; Antimalarials; Atovaquone; Biological Availability; Dose-Response Relationship, Drug; Drug Combinations; Female; Genotype; Humans; In Vitro Techniques; Male; Middle Aged; Naphthoquinones; Phenotype; Proguanil; Time Factors; Triazines | 2002 |
Pregnancy and use of oral contraceptives reduces the biotransformation of proguanil to cycloguanil.
Topics: Antimalarials; Biotransformation; Case-Control Studies; Cohort Studies; Contraceptives, Oral, Hormonal; Female; Humans; Malaria, Falciparum; Pregnancy; Pregnancy Complications, Parasitic; Pregnancy Trimester, Third; Proguanil; Thailand; Triazines | 2003 |
Concordance between proguanil phenotype and CYP2C19 genotype in Chinese.
Topics: Adult; Alleles; Antimetabolites; Aryl Hydrocarbon Hydroxylases; Asian People; Biguanides; Cytochrome P-450 CYP2C19; Female; Genotype; Humans; Male; Middle Aged; Mixed Function Oxygenases; Phenotype; Proguanil; Triazines | 2003 |
The pharmacokinetics and pharmacodynamics of atovaquone and proguanil for the treatment of uncomplicated falciparum malaria in third-trimester pregnant women.
Topics: Adolescent; Adult; Antimalarials; Atovaquone; Drug Combinations; Female; Humans; Malaria, Falciparum; Naphthoquinones; Pregnancy; Proguanil; Thailand; Triazines; Zambia | 2005 |
Effect of honey on CYP3A4, CYP2D6 and CYP2C19 enzyme activity in healthy human volunteers.
Topics: Administration, Oral; Adult; Aryl Hydrocarbon Hydroxylases; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Dextromethorphan; Dextrorphan; Honey; Humans; Hydrocortisone; India; Male; Mixed Function Oxygenases; Proguanil; Triazines | 2007 |
OCT1 Deficiency Affects Hepatocellular Concentrations and Pharmacokinetics of Cycloguanil, the Active Metabolite of the Antimalarial Drug Proguanil.
Topics: Adolescent; Adult; Antimalarials; Dose-Response Relationship, Drug; Female; HEK293 Cells; Hepatocytes; Humans; Male; Middle Aged; Octamer Transcription Factor-1; Proguanil; Triazines; Young Adult | 2019 |
Effects of proton pump inhibitors, esomeprazole and vonoprazan, on the disposition of proguanil, a CYP2C19 substrate, in healthy volunteers.
Topics: Adult; Area Under Curve; Atovaquone; Chromatography, Liquid; Cytochrome P-450 CYP2C19; Drug Combinations; Esomeprazole; Humans; Male; Proguanil; Proton Pump Inhibitors; Pyrroles; Sulfonamides; Tandem Mass Spectrometry; Triazines; Young Adult | 2019 |
Evaluation of CYP2C19-Mediated Pharmacokinetic Drug Interaction of Tegoprazan, Compared with Vonoprazan or Esomeprazole.
Topics: Atovaquone; Cross-Over Studies; Cytochrome P-450 CYP2C19; Drug Interactions; Esomeprazole; Humans; Proguanil; Reducing Agents | 2023 |
169 other study(ies) available for cycloguanil and proguanil
| Article | Year |
|---|---|
In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.
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 |
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
Topics: Antiparasitic Agents; Molecular Structure; Neural Networks, Computer; Parasitic Diseases; Quantitative Structure-Activity Relationship; Species Specificity; Thermodynamics | 2010 |
Novel biguanide-based derivatives scouted as TAAR1 agonists: Synthesis, biological evaluation, ADME prediction and molecular docking studies.
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.
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 |
Plasmodium falciparum: rapid detection of dihydrofolate reductase mutations that confer resistance to cycloguanil and pyrimethamine.
Topics: Animals; Base Sequence; Drug Resistance; Molecular Sequence Data; Mutation; Plasmodium falciparum; Polymerase Chain Reaction; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines | 1992 |
The activation of the biguanide antimalarial proguanil co-segregates with the mephenytoin oxidation polymorphism--a panel study.
Topics: Adult; Female; Humans; Male; Mephenytoin; Oxidation-Reduction; Phenotype; Polymorphism, Genetic; Proguanil; Reference Values; Sparteine; Triazines | 1991 |
Dapsone in low doses prevents Pneumocystis carinii pneumonia in the rat model.
Topics: Administration, Oral; Animals; Dapsone; Diet; Disease Models, Animal; Immune Tolerance; Male; Pneumonia, Pneumocystis; Proguanil; Random Allocation; Rats; Rats, Inbred Strains; Triazines | 1991 |
Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses.
Topics: Adult; Aged; Antimalarials; Chromatography, High Pressure Liquid; Erythrocytes; Female; Humans; Male; Middle Aged; Proguanil; Triazines | 1991 |
In vitro and in vivo susceptibility of Plasmodium falciparum isolates from Liberia to pyrimethamine, cycloguanil and chlorcycloguanil.
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.
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.
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 |
Multiple-dose kinetics in healthy volunteers and in vitro antimalarial activity of proguanil plus dapsone.
Topics: Adult; Animals; Anti-Infective Agents; Dapsone; Drug Administration Schedule; Drug Resistance; Drug Synergism; Drug Therapy, Combination; Half-Life; Humans; Male; Plasmodium falciparum; Proguanil; Time Factors; Triazines | 1990 |
Multiple-dose pharmacokinetic study of proguanil and cycloguanil following 12-hourly administration of 100 mg proguanil hydrochloride.
Topics: Adult; Drug Administration Schedule; Humans; Male; Proguanil; Triazines | 1990 |
The pharmacokinetics and activation of proguanil in man: consequences of variability in drug metabolism.
Topics: Biotransformation; Chromatography, High Pressure Liquid; Humans; Proguanil; Spectrophotometry, Ultraviolet; Triazines | 1990 |
Structure of cycloguanil hydrochloride by neutron diffraction.
Topics: Chemical Phenomena; Chemistry, Physical; Crystallization; Crystallography; Molecular Structure; Neutrons; Proguanil; Triazines | 1989 |
Inter-subject variability in the metabolism of proguanil to the active metabolite cycloguanil in man.
Topics: Adolescent; Adult; Child; Female; Humans; Kenya; Male; Proguanil; Triazines; United Kingdom | 1989 |
In-vitro activity of dapsone and two potentiators against Mycobacterium avium complex.
Topics: Acquired Immunodeficiency Syndrome; Anti-Bacterial Agents; Dapsone; Drug Synergism; Humans; Microbial Sensitivity Tests; Mycobacterium avium Complex; Mycobacterium avium-intracellulare Infection; Proguanil; Sulfamethazine; Triazines | 1989 |
The pharmacokinetics of proguanil in human subjects following a single oral dose.
Topics: Administration, Oral; Chromatography, High Pressure Liquid; Humans; Kinetics; Male; Proguanil; Triazines | 1987 |
A sensitive bioassay for serum cycloguanil using Plasmodium falciparum in vitro.
Topics: Adult; Animals; Biological Assay; Humans; Male; Plasmodium falciparum; Predictive Value of Tests; Proguanil; Triazines | 1988 |
Superior antimalarial activity of proguanil to cycloguanil after in vitro bioconversion.
Topics: Animals; Antimalarials; Biotransformation; Drug Resistance; Plasmodium falciparum; Proguanil; Triazines | 1988 |
Malaria breakthrough despite chlorproguanil chemoprophylaxis in an area without antifol resistance.
Topics: Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; Humans; Malaria; Plasmodium falciparum; Proguanil; Triazines | 1988 |
Steady-state kinetics of proguanil and its active metabolite, cycloguanil, in man.
Topics: Administration, Oral; Adult; Half-Life; Humans; Male; Metabolic Clearance Rate; Proguanil; Triazines | 1988 |
Selective inhibition of Leishmania dihydrofolate reductase and Leishmania growth by 5-benzyl-2,4-diaminopyrimidines.
Topics: Animals; Antimalarials; Folic Acid Antagonists; Leishmania tropica; Proguanil; Pyrimethamine; Pyrimidines; Triazines; Trimethoprim | 1988 |
Pharmacokinetics of chlorproguanil in man after a single oral dose of Lapudrine.
Topics: Administration, Oral; Adult; Half-Life; Humans; Male; Metabolic Clearance Rate; Proguanil; Triazines | 1988 |
Synergistic antimalarial activity of dapsone/dihydrofolate reductase inhibitors and the interaction of antifol, antipyrimidine and antipurine combinations against Plasmodium falciparum in vitro.
Topics: Animals; Antimalarials; Antimetabolites; Dapsone; Drug Synergism; Plasmodium falciparum; Proguanil; Ribonucleosides; Triazines | 1987 |
Single dose pharmacokinetics of proguanil and its metabolites in healthy subjects.
Topics: Adult; Erythrocytes; Humans; Male; Proguanil; Triazines | 1987 |
Chlorproguanil and chlorcycloguanil concentrations in human plasma and urine after Lapudrine administration.
Topics: Adult; Antimalarials; Chromatography, High Pressure Liquid; Half-Life; Humans; Male; Proguanil; Triazines | 1987 |
Analogues of N-benzyloxydihydrotriazines: in vitro antimalarial activity against Plasmodium falciparum.
Topics: Antimalarials; Chloroquine; Drug Resistance, Microbial; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 1986 |
Response of Plasmodium falciparum to dihydrofolate reductase inhibitors in Malindi, Kenya.
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.
Topics: Animals; Antiprotozoal Agents; Drug Interactions; Folic Acid Antagonists; Hypoxanthines; Naphthoquinones; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 1986 |
Determination of proguanil and its metabolites cycloguanil and 4-chlorophenylbiguanide in plasma, whole blood and urine by high-performance liquid chromatography.
Topics: Biguanides; Chromatography, High Pressure Liquid; Humans; Kinetics; Proguanil; Triazines | 1987 |
Human pharmacokinetics of proguanil and its metabolites.
Topics: Adult; Biguanides; Chemical Phenomena; Chemistry; Chromatography, High Pressure Liquid; Erythrocytes; Female; Half-Life; Humans; Kinetics; Male; Proguanil; Triazines | 1987 |
Effect of oral proguanil on human lymphocyte proliferation.
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.
Topics: Chemical Phenomena; Chemistry; Chromatography, High Pressure Liquid; Humans; Proguanil; Pyrimethamine; Spectrophotometry, Ultraviolet; Triazines | 1986 |
High-performance liquid chromatographic method for the determination of proguanil and cycloguanil in biological fluids.
Topics: Chromatography, High Pressure Liquid; Female; Humans; Male; Proguanil; Spectrophotometry, Ultraviolet; Triazines | 1986 |
Effect of proguanil and cycloguanil on human lymphocytes in vitro.
Topics: Humans; Leucovorin; Lymphocyte Activation; Proguanil; Thymidine; Triazines | 1985 |
Evaluation of sporontocidal compounds using Plasmodium falciparum gametocytes produced in vitro.
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.
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.
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.
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.
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.
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.
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.
Topics: Antimalarials; Chemotaxis, Leukocyte; Chloroquine; Drug Combinations; Humans; Neutrophils; Proguanil; Pyrimethamine; Quinine; Sulfadoxine; Tetracycline; Triazines | 1983 |
Crystallographic and molecular-orbital studies on the geometry of antifolate drugs.
Topics: Chemical Phenomena; Chemistry; Crystallography; Folic Acid Antagonists; Proguanil; Pyrimidines; Quinazolines; Triazines | 1980 |
Sustained-release implants in the chemotherapy of experimental rodent malaria I. A comparison of the effects of some antimalarials in polydimethylsiloxane matrices.
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.
Topics: Animals; Biodegradation, Environmental; Drug Implants; Malaria; Male; Mice; Mice, Inbred Strains; Plasmodium berghei; Proguanil; Pyrimethamine; Sulfadiazine; Triazines | 1981 |
High-performance liquid chromatography of proguanil, cycloguanil and 4-chlorophenylbiguanide using hydrophobic pairing ion and its application to serum assay.
Topics: Animals; Biguanides; Cattle; Chromatography, High Pressure Liquid; Humans; Proguanil; Surface-Active Agents; Triazines | 1980 |
Metabolic disposition of proguanil in extensive and poor metabolisers of S-mephenytoin 4'-hydroxylation recruited from an Indonesian population.
Topics: Adult; Biguanides; Chromatography, High Pressure Liquid; Cohort Studies; Female; Half-Life; Humans; Hydroxylation; Indonesia; Male; Mephenytoin; Middle Aged; Polymorphism, Genetic; Proguanil; Regression Analysis; Triazines | 1995 |
Point mutations in the dihydrofolate reductase-thymidylate synthase gene and pyrimethamine and cycloguanil resistance in Plasmodium falciparum.
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.
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 |
A statistical analysis of the antimalarial activity of proguanil and cycloguanil in human volunteers.
Topics: Adolescent; Adult; Animals; Antimalarials; Biological Assay; Chromatography, High Pressure Liquid; Humans; Malaria; Male; Plasmodium falciparum; Proguanil; Regression Analysis; Triazines | 1994 |
In vitro proguanil activation to cycloguanil by human liver microsomes is mediated by CYP3A isoforms as well as by S-mephenytoin hydroxylase.
Topics: Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Humans; Isoenzymes; Microsomes, Liver; Mixed Function Oxygenases; Proguanil; Triazines | 1994 |
In vitro susceptibility of Cambodian isolates of Plasmodium falciparum to halofantrine, pyronaridine and artemisinin derivatives.
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 effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii.
Topics: Animals; Artemisinins; Female; Mefloquine; Mice; Primaquine; Proguanil; Quinine; Sesquiterpenes; Sulfadiazine; Toxoplasma; Triazines; Trifluoperazine; Uracil; Verapamil | 1994 |
In vitro activity of pyrimethamine, cycloguanil, and other antimalarial drugs against African isolates and clones of Plasmodium falciparum.
Topics: Africa; Animals; Antimalarials; Chloroquine; Drug Resistance; Humans; Mefloquine; Phenanthrenes; Plasmodium falciparum; Proguanil; Pyrimethamine; Quinine; Triazines | 1994 |
Oxidative activation of proguanil and dapsone acetylation in Thai soldiers.
Topics: Acetylation; Biotransformation; Chromatography, High Pressure Liquid; Dapsone; Humans; Malaria; Military Personnel; Oxidation-Reduction; Polymorphism, Genetic; Proguanil; Thailand; Triazines | 1994 |
The multiple dose pharmacokinetics of proguanil.
Topics: Adult; Biguanides; Chromatography, High Pressure Liquid; Cytochrome P-450 Enzyme System; Female; Humans; Male; Polymorphism, Genetic; Proguanil; Triazines | 1993 |
PS-15: a potent, orally active antimalarial from a new class of folic acid antagonists.
Topics: Administration, Oral; Animals; Antimalarials; Aotus trivirgatus; Atovaquone; Drug Synergism; Folic Acid Antagonists; Imides; Injections, Subcutaneous; Malaria, Falciparum; Mice; Naphthoquinones; Phenyl Ethers; Plasmodium falciparum; Proguanil; Sulfamethoxazole; Triazines | 1993 |
Proguanil metabolism is determined by the mephenytoin oxidation polymorphism in Vietnamese living in Denmark.
Topics: Administration, Oral; Adult; Biguanides; Denmark; Female; Humans; Male; Mephenytoin; Middle Aged; Oxidation-Reduction; Phenotype; Polymorphism, Genetic; Proguanil; Sparteine; Triazines; Vietnam | 1993 |
Single dose pharmacokinetics of proguanil and its metabolites in pregnancy.
Topics: Biguanides; Female; Humans; Malaria; Male; Pregnancy; Pregnancy Complications, Parasitic; Pregnancy Trimester, Third; Proguanil; Triazines | 1993 |
In vitro activity of cycloguanil against African isolates of Plasmodium falciparum.
Topics: Animals; Erythrocytes; Humans; Liver; Malaria, Falciparum; Microbial Sensitivity Tests; Plasmodium falciparum; Proguanil; Triazines | 1993 |
Human pharmacokinetics of chloroquine and proguanil delivered in a single capsule for malaria chemoprophylaxis.
Topics: Adult; Antimalarials; Chloroquine; Drug Combinations; Drug Therapy, Combination; Female; Humans; Malaria; Male; Middle Aged; Proguanil; Triazines | 1995 |
Plasmodium falciparum: molecular characterization of multidrug-resistant Cambodian isolates.
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 |
Simultaneous measurement of proguanil and its metabolites in human plasma and urine by reversed-phase high-performance liquid chromatography, and its preliminary application in relation to genetically determined S-mephenytoin 4'-hydroxylation status.
Topics: Adult; Antimalarials; Biguanides; Chromatography, High Pressure Liquid; Humans; Hydroxylation; Male; Mephenytoin; Middle Aged; Phenotype; Proguanil; Triazines | 1996 |
Determination of proguanil and metabolites in small sample volumes of whole blood stored on filter paper by high-performance liquid chromatography.
Topics: Antimalarials; Biguanides; Blood Specimen Collection; Calibration; Chromatography, High Pressure Liquid; Drug Stability; Humans; Proguanil; Triazines | 1995 |
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.
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.
Topics: Animals; Clone Cells; Drug Resistance; Folic Acid Antagonists; Humans; Methotrexate; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 1996 |
Correlation between proguanil and metabolites in plasma and saliva.
Topics: Antimalarials; Biguanides; Chromatography, High Pressure Liquid; Humans; Proguanil; Saliva; Triazines | 1995 |
Effects of omeprazole and cimetidine on the urinary metabolic ratio of proguanil in healthy volunteers.
Topics: Adult; Aryl Hydrocarbon Hydroxylases; Cimetidine; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Female; Humans; Male; Mixed Function Oxygenases; Omeprazole; Proguanil; 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.
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.
Topics: Animals; Antimalarials; Clone Cells; Drug Resistance; Folic Acid Antagonists; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 1996 |
Inhibition by omeprazole of proguanil metabolism: mechanism of the interaction in vitro and prediction of in vivo results from the in vitro experiments.
Topics: Aryl Hydrocarbon Hydroxylases; Biotransformation; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Humans; Kinetics; Male; Microsomes, Liver; Mixed Function Oxygenases; Omeprazole; Proguanil; Reference Values; Triazines | 1997 |
Antifolate-resistant mutants of Plasmodium falciparum dihydrofolate reductase.
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.
Topics: Animals; Antimalarials; Atovaquone; Drug Interactions; Folic Acid; Humans; Leucovorin; Naphthoquinones; Plasmodium falciparum; Proguanil; Purine Nucleotides; Pyrimethamine; Pyrimidine Nucleotides; Triazines | 1997 |
Ex vivo antimalarial activity of proguanil combined with dapsone against cycloguanil-resistant Plasmodium falciparum isolates.
Topics: Animals; Antimalarials; Dapsone; Drug Resistance; Drug Therapy, Combination; Humans; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Triazines | 1997 |
In vitro sensitivity of Plasmodium falciparum to anti-folinic agents (trimethoprim, pyrimethamine, cycloguanil): a study of 29 African strains.
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 |
In vitro activities of the biguanide PS-15 and its metabolite, WR99210, against cycloguanil-resistant Plasmodium falciparum isolates from Thailand.
Topics: Animals; Antimalarials; Drug Resistance, Microbial; Folic Acid Antagonists; Malaria; Plasmodium falciparum; Prodrugs; Proguanil; Saimiri; Thailand; Triazines | 1997 |
Plasmodium falciparum: asparagine mutant at residue 108 of dihydrofolate reductase is an optimal antifolate-resistant single mutant.
Topics: Animals; Asparagine; Drug Resistance; Folic Acid Antagonists; Genes, Protozoan; Genes, Synthetic; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Recombinant Proteins; Tetrahydrofolate Dehydrogenase; Triazines | 1997 |
Proguanil resistance in Plasmodium falciparum African isolates: assessment by mutation-specific polymerase chain reaction and in vitro susceptibility testing.
Topics: Africa; Amino Acid Substitution; Animals; Asparagine; Codon; DNA, Protozoan; Drug Resistance, Microbial; Humans; Malaria, Falciparum; Microbial Sensitivity Tests; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Proguanil; Sequence Analysis, DNA; Serine; 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.
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.
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 |
Hepatic cytochrome P450 CYP2C activity in psoriasis: studies using proguanil as a probe compound.
Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Antimalarials; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Female; Folic Acid Antagonists; Humans; In Vitro Techniques; Liver; Male; Microsomes, Liver; Middle Aged; Mixed Function Oxygenases; Phenotype; Proguanil; Prospective Studies; Psoriasis; Severity of Illness Index; Triazines; Vitamin A | 1998 |
Improved validated assay for the determination of proguanil and its metabolites in plasma, whole blood, and urine using solid-phase extraction and high-performance liquid chromatography.
Topics: Antimalarials; Biguanides; Biological Assay; Chromatography, High Pressure Liquid; Drug Monitoring; Folic Acid Antagonists; Humans; Proguanil; Reproducibility of Results; Sensitivity and Specificity; Triazines | 1998 |
Comparative effects of cycloguanil and WR99210 in human leukaemia cells and intra-erythrocytic Plasmodium.
Topics: Animals; Antimalarials; Erythrocytes; Humans; Leukemia; Nucleotides; Plasmodium falciparum; Prodrugs; Proguanil; Triazines; Tumor Cells, Cultured | 1998 |
[Considering disparities in resistance of Plasmodium falciparum in Africa in chemoprevention decisions].
Topics: Africa; Animals; Antimalarials; Chloroquine; Cross-Cultural Comparison; Dose-Response Relationship, Drug; Drug Resistance, Multiple; Folic Acid Antagonists; Humans; Malaria, Falciparum; Mefloquine; Plasmodium falciparum; Proguanil; Seasons; Travel; Triazines | 1998 |
Relationship between proguanil metabolic ratio and CYP2C19 genotype in a Caucasian population.
Topics: Adolescent; Adult; Aryl Hydrocarbon Hydroxylases; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Dextromethorphan; Female; Gene Frequency; Genotype; Humans; Male; Middle Aged; Mixed Function Oxygenases; Mutation; Proguanil; Statistics as Topic; Triazines; White People | 1998 |
Cycloguanil and its parent compound proguanil demonstrate distinct activities against Plasmodium falciparum malaria parasites transformed with human dihydrofolate reductase.
Topics: Animals; Antimalarials; Folic Acid Antagonists; Genetic Complementation Test; Humans; Hypoxanthine; Inhibitory Concentration 50; Methotrexate; Mutation; Plasmodium falciparum; Proguanil; Tetrahydrofolate Dehydrogenase; Triazines | 1998 |
Improved method for the simultaneous determination of proguanil and its metabolites by high-performance liquid chromatography and solid-phase extraction of 100-microl capillary blood samples dried on sampling paper.
Topics: Antimalarials; Biguanides; Capillaries; Chromatography, High Pressure Liquid; Humans; Paper; Proguanil; Reproducibility of Results; Sensitivity and Specificity; Triazines | 1998 |
Intrinsic efficacy of proguanil against falciparum and vivax malaria independent of the metabolite cycloguanil.
Topics: Adolescent; Antimalarials; Aryl Hydrocarbon Hydroxylases; Child; Child, Preschool; Cytochrome P-450 CYP2C19; Cytochrome P-450 Enzyme System; Genotype; Humans; Infant; Malaria, Falciparum; Malaria, Vivax; Mixed Function Oxygenases; Proguanil; Tetrahydrofolate Dehydrogenase; Triazines | 1999 |
[Resistance to chloroquine and cycloguanil of Plasmodium falciparum in patients arriving in France after travel in Africa without chemoprophylaxis].
Topics: Africa; Animals; Antimalarials; Chloroquine; Codon; Drug Resistance, Multiple; Folic Acid Antagonists; France; Humans; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Seasons; Tetrahydrofolate Dehydrogenase; Travel; Triazines | 1998 |
[In vitro sensitivity of Plasmodium falciparum isolates from Gabon to chloroquine and cycloguanil].
Topics: Adolescent; Animals; Antimalarials; Child; Child, Preschool; Chloroquine; Drug Resistance; Gabon; Humans; Infant; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Triazines | 1999 |
Comparison of (S)-mephenytoin and proguanil oxidation in vitro: contribution of several CYP isoforms.
Topics: Adult; Aged; Antibodies, Monoclonal; Anticonvulsants; Antimetabolites; Cytochrome P-450 Enzyme System; Enzyme Inhibitors; Female; Folic Acid Antagonists; Genotype; Humans; In Vitro Techniques; Isoenzymes; Male; Mephenytoin; Microsomes, Liver; Middle Aged; Oxidation-Reduction; Proguanil; Triazines | 1999 |
Identification and analysis of dihydrofolate reductase alleles from Plasmodium falciparum present at low frequency in polyclonal patient samples.
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 |
Increased incidence of cycloguanil resistance in malaria cases entering France from Africa, determined as point mutations in the parasites' dihydrofolate-reductase genes.
Topics: Africa; Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; France; Genes, Protozoan; Humans; Malaria, Falciparum; Plasmodium falciparum; Point Mutation; Polymerase Chain Reaction; Polymorphism, Restriction Fragment Length; Proguanil; Tetrahydrofolate Dehydrogenase; Triazines | 1999 |
Phenotypes and genotypes for CYP2D6 and CYP2C19 in a black Tanzanian population.
Topics: Adult; Alleles; Aryl Hydrocarbon Hydroxylases; Black People; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2D6; Cytochrome P-450 Enzyme System; Female; Genetic Variation; Genetics, Population; Genotype; Humans; Male; Mephenytoin; Mixed Function Oxygenases; Phenotype; Proguanil; Sparteine; Tanzania; Triazines | 1999 |
[Variability of in vitro activity of proguanil and cycloguanil on erythrocyte stages of Plasmodium falciparum as a function of culture conditions].
Topics: Animals; Antimalarials; Cells, Cultured; Chloroquine; Culture Media; Drug Resistance; Erythrocytes; Humans; Plasmodium falciparum; Proguanil; Triazines | 1999 |
Gametocytocidal activity of pyronaridine and DNA topoisomerase II inhibitors against multidrug-resistant Plasmodium falciparum in vitro.
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.
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.
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.
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 |
Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.
Topics: Amino Acid Substitution; Animals; Antimalarials; Drug Resistance; Folic Acid Antagonists; Mutation; Plasmodium falciparum; Proguanil; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines | 2000 |
Genome comparison of progressively drug resistant Plasmodium falciparum lines derived from drug sensitive clone.
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 |
Analysis of proguanil and its metabolites by application of the sweeping technique in micellar electrokinetic chromatography.
Topics: Biguanides; Chromatography, Micellar Electrokinetic Capillary; Proguanil; Sensitivity and Specificity; Triazines | 2001 |
In vitro proguanil activation to cycloguanil is mediated by CYP2C19 and CYP3A4 in adult Chinese liver microsomes.
Topics: Adult; Antimalarials; Aryl Hydrocarbon Hydroxylases; Asian People; Biotransformation; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Humans; In Vitro Techniques; Microsomes, Liver; Middle Aged; Mixed Function Oxygenases; Proguanil; Triazines; Troleandomycin | 2000 |
Homology modeling of wild type and pyrimethamine/cycloguanil-cross resistant mutant type Plasmodium falciparum dihydrofolate reductase. A model for antimalarial chemotherapy resistance.
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.
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.
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.
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 |
Synthesis of solution-phase combinatorial library of 4,6-diamino-1,2-dihydro-1,3,5-triazine and identification of new leads against A16V+S108T mutant dihydrofolate reductase of Plasmodium falciparum.
Topics: Amino Acid Substitution; Animals; Antimalarials; Biguanides; Combinatorial Chemistry Techniques; Cyclization; Folic Acid Antagonists; Mutation; Plasmodium falciparum; Proguanil; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines | 2003 |
[Gene point mutation in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum].
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 |
Profile and evolution of the chemosusceptibility of falciparum malaria imported into France in 2000.
Topics: Adolescent; Adult; Aged; Animals; Antimalarials; Child; Child, Preschool; Chloroquine; Drug Resistance; Female; France; Humans; Infant; Malaria, Falciparum; Male; Mefloquine; Middle Aged; Plasmodium falciparum; Proguanil; Quinine; Triazines | 2002 |
Different mutation patterns of atovaquone resistance to Plasmodium falciparum in vitro and in vivo: rapid detection of codon 268 polymorphisms in the cytochrome b as potential in vivo resistance marker.
Topics: Animals; Antimalarials; Antiprotozoal Agents; Atovaquone; Codon; Drug Resistance; Electron Transport Complex III; Genetic Markers; Humans; Malaria, Falciparum; Mutation; Naphthoquinones; Plasmodium falciparum; Polymerase Chain Reaction; Polymorphism, Genetic; Polymorphism, Restriction Fragment Length; Proguanil; Triazines | 2003 |
In vitro sensitivity of Plasmodium falciparum to amodiaquine compared with other major antimalarials in Madagascar.
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.
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.
Topics: Animals; Antimalarials; Dihydropteroate Synthase; DNA, Protozoan; Gabon; Genotype; Humans; Plasmodium falciparum; Proguanil; Pyrimethamine; Sulfadoxine; Tetrahydrofolate Dehydrogenase; Triazines | 2003 |
Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.
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 |
Susceptibility of Plasmodium falciparum to the drugs used to treat severe malaria (quinine) and to prevent malaria (mefloquine, cycloguanil) in Comoros Union and Madagascar.
Topics: Animals; Antimalarials; Comoros; Drug Resistance; Humans; In Vitro Techniques; Madagascar; Malaria, Falciparum; Mefloquine; Plasmodium falciparum; Proguanil; Quinine; Triazines | 2004 |
Short communication: Prevalence of mutations associated with resistance to atovaquone and to the antifolate effect of proguanil in Plasmodium falciparum isolates from northern Ghana.
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 |
In vitro recrudescence of Plasmodium falciparum parasites suppressed to dormant state by atovaquone alone and in combination with proguanil.
Topics: Animals; Antimalarials; Atovaquone; Culture Media; Cytochrome b Group; Dose-Response Relationship, Drug; Drug Resistance; Drug Therapy, Combination; Humans; Malaria, Falciparum; Naphthoquinones; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Recurrence; Triazines | 2005 |
Novel alleles of Plasmodium falciparum dhfr that confer resistance to chlorcycloguanil.
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 |
Syntheses of 2,4,6-trisubstituted triazines as antimalarial agents.
Topics: Animals; Antimalarials; Blood; Humans; Microbial Sensitivity Tests; Plasmodium falciparum; Proguanil; Structure-Activity Relationship; Triazines | 2005 |
The chemotherapy of rodent malaria. LXII. Drug combinations to impede the selection of drug resistance, part 5: rates of development of resistance to some inhibitors of folate metabolism and to artesunate.
Topics: Animals; Antimalarials; Artemisinins; Artesunate; Dapsone; Drug Resistance; Drug Therapy, Combination; Folic Acid Antagonists; Malaria, Falciparum; Male; Mice; Parasitemia; Plasmodium berghei; Plasmodium chabaudi; Plasmodium yoelii; Proguanil; Sesquiterpenes; Triazines | 2004 |
Stoichiometric selection of tight-binding inhibitors by wild-type and mutant forms of malarial (Plasmodium falciparum) dihydrofolate reductase.
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.
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 |
2,4-diaminopteridine-based compounds as precursors for de novo synthesis of antifolates: a novel class of antimalarials.
Topics: Animals; Antimalarials; Dapsone; Dihydropteroate Synthase; Drug Combinations; Drug Synergism; Folic Acid Antagonists; Plasmodium; Proguanil; Pteridines; Saccharomyces cerevisiae; Tetrahydrofolate Dehydrogenase; Triazines | 2005 |
Plasmodium falciparum: interaction of shikimate analogues with antimalarial drugs.
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.
Topics: Animals; Antimalarials; Clone Cells; Drug Resistance; Folic Acid Antagonists; In Vitro Techniques; Malaysia; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 2005 |
Sensitive method for the quantitative determination of proguanil and its metabolites in rat blood and plasma by liquid chromatography-mass spectrometry.
Topics: Administration, Oral; Animals; Antimalarials; Biguanides; Calibration; Chromatography, High Pressure Liquid; Drug Stability; Freezing; Injections, Intravenous; Proguanil; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; Triazines | 2006 |
Multiple synergistic interactions between atovaquone and antifolates against Plasmodium falciparum in vitro: a rational basis for combination therapy.
Topics: Animals; Antimalarials; Atovaquone; Dapsone; Drug Synergism; Drug Therapy, Combination; Folic Acid Antagonists; Naphthoquinones; Plasmodium falciparum; Proguanil; Triazines | 2006 |
Population pharmacokinetic and pharmacodynamic modelling of the antimalarial chemotherapy chlorproguanil/dapsone.
Topics: Adolescent; Adult; Animals; Antimalarials; Child; Child, Preschool; Dapsone; Humans; Infant; Malaria, Falciparum; Middle Aged; Plasmodium falciparum; Proguanil; Prospective Studies; Triazines | 2006 |
Amino acid mutations in Plasmodium vivax DHFR and DHPS from several geographical regions and susceptibility to antifolate drugs.
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 |
Simultaneous determination of monodesethylchloroquine, chloroquine, cycloguanil and proguanil on dried blood spots by reverse-phase liquid chromatography.
Topics: Antimalarials; Calibration; Chloroquine; Chromatography, High Pressure Liquid; Humans; Indicators and Reagents; Proguanil; Quality Control; Reference Standards; Reproducibility of Results; Spectrophotometry, Ultraviolet; Triazines | 2007 |
The role of tryptophan-48 in catalysis and binding of inhibitors of Plasmodium falciparum dihydrofolate reductase.
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.
Topics: Animals; Antimalarials; Drug Resistance; Drug Resistance, Multiple; Kinetics; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Tetrahydrofolate Dehydrogenase; Triazines | 2007 |
Role of specific cytochrome P450 isoforms in the conversion of phenoxypropoxybiguanide analogs in human liver microsomes to potent antimalarial dihydrotriazines.
Topics: Antibodies, Monoclonal; Antimalarials; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Humans; Microsomes, Liver; Prodrugs; Proguanil; Protein Isoforms; Recombinant Proteins; Triazines | 2008 |
Effect of folate derivatives on the activity of antifolate drugs used against malaria and cancer.
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.
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 |
Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents.
Topics: Aminoquinolines; Animals; Antimalarials; Chemistry, Pharmaceutical; Chloroquine; Drug Design; Erythrocytes; Humans; Inhibitory Concentration 50; Models, Chemical; Parasitic Sensitivity Tests; Plasmodium falciparum; Plasmodium yoelii; Proguanil; Triazines | 2008 |
Interactions between cycloguanil derivatives and wild type and resistance-associated mutant Plasmodium falciparum dihydrofolate reductases.
Topics: Algorithms; Amino Acid Substitution; Animals; Antimalarials; Catalytic Domain; Drug Design; Drug Resistance; Folic Acid Antagonists; Hydrogen Bonding; Models, Molecular; Plasmodium falciparum; Proguanil; Protein Binding; Quantum Theory; Static Electricity; Tetrahydrofolate Dehydrogenase; Thermodynamics; Triazines | 2009 |
A novel in silico approach to drug discovery via computational intelligence.
Topics: Algorithms; Antimalarials; Artificial Intelligence; Computer Simulation; Crystallography, X-Ray; Drug Design; Drug Evaluation, Preclinical; Folic Acid Antagonists; Molecular Conformation; Neural Networks, Computer; Pharmaceutical Preparations; Proguanil; Quantitative Structure-Activity Relationship; Regression Analysis; Reproducibility of Results; Small Molecule Libraries; Tetrahydrofolate Dehydrogenase; Triazines | 2009 |
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.
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 |
Structure-activity relationship and comparative docking studies for cycloguanil analogs as PfDHFR-TS inhibitors.
Topics: Animals; Antimalarials; Drug Resistance; Hydrophobic and Hydrophilic Interactions; Models, Molecular; Molecular Structure; Mutation; Plasmodium falciparum; Proguanil; Protein Binding; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines | 2009 |
Effects of genetic variation at the CYP2C19/CYP2C9 locus on pharmacokinetics of chlorcycloguanil in adult Gambians.
Topics: Adolescent; Adult; Alleles; Antimalarials; Area Under Curve; Aryl Hydrocarbon Hydroxylases; Biotransformation; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2C9; DNA; Female; Gambia; Gene Frequency; Genetic Variation; Genotype; Haplotypes; Humans; Male; Middle Aged; Proguanil; Triazines; Young Adult | 2009 |
3D-QSAR analysis of cycloguanil derivatives as inhibitors of A16V + S108T mutant Plasmodium falciparum dihydrofolate reductase enzyme.
Topics: Animals; Catalytic Domain; Crystallography, X-Ray; Enzyme Inhibitors; Folic Acid Antagonists; Hydrophobic and Hydrophilic Interactions; Inhibitory Concentration 50; Models, Molecular; Mutant Proteins; Parasitic Sensitivity Tests; Plasmodium falciparum; Proguanil; Protein Structure, Secondary; Quantitative Structure-Activity Relationship; Static Electricity; Tetrahydrofolate Dehydrogenase; Thermodynamics; Triazines | 2009 |
Shape- and chemical feature-based 3D-pharmacophore model generation and virtual screening: identification of potential leads for P. falciparum DHFR enzyme inhibition.
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 |
Quantitative structure-activity relationships for cycloguanil analogs as PfDHFR inhibitors using mathematical molecular descriptors.
Topics: Antiprotozoal Agents; Computer Simulation; Folic Acid Antagonists; Models, Statistical; Plasmodium falciparum; Proguanil; Quantitative Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Triazines | 2010 |
Exploring QSAR, pharmacophore mapping and docking studies and virtual library generation for cycloguanil derivatives as PfDHFR-TS inhibitors.
Topics: Antimalarials; Drug Design; Enzyme Inhibitors; Models, Molecular; Molecular Structure; Plasmodium falciparum; Proguanil; Quantitative Structure-Activity Relationship; Small Molecule Libraries; Stereoisomerism; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines | 2011 |
Fitness trade-offs in the evolution of dihydrofolate reductase and drug resistance in Plasmodium falciparum.
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.
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 |
Combined spatial limitation around residues 16 and 108 of Plasmodium falciparum dihydrofolate reductase explains resistance to cycloguanil.
Topics: Antimalarials; Drug Resistance; Folic Acid Antagonists; Mutation; Plasmodium falciparum; Proguanil; Tetrahydrofolate Dehydrogenase; Triazines | 2012 |
Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.
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.
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 |
Effects of metformin and other biguanides on oxidative phosphorylation in mitochondria.
Topics: Animals; Antimalarials; Antineoplastic Agents; Biguanides; Cattle; Diabetes Mellitus, Type 2; Electron Transport Complex I; Hep G2 Cells; Humans; Metformin; Mitochondria, Heart; Mitochondria, Liver; Mitochondrial Proton-Translocating ATPases; Oxidative Phosphorylation; Plasmodium; Proguanil; Rats; Reperfusion Injury; Triazines | 2014 |
Importance of cytochromes in cyclization reactions: quantum chemical study on a model reaction of proguanil to cycloguanil.
Topics: Cyclization; Cytochromes; Models, Chemical; Proguanil; Quantum Theory; Triazines | 2014 |
Metabolic Dysregulation Induced in Plasmodium falciparum by Dihydroartemisinin and Other Front-Line Antimalarial Drugs.
Topics: Antimalarials; Artemisinins; Atovaquone; Chloroquine; Fosfomycin; Gas Chromatography-Mass Spectrometry; Hemoglobins; Inhibitory Concentration 50; Methylene Blue; Naphthyridines; Plasmodium falciparum; Proguanil; Triazines | 2016 |
Cytogenetic and oxidative status of human lymphocytes after exposure to clinically relevant concentrations of antimalarial drugs atovaquone and proguanil hydrochloride in vitro.
Topics: Adult; Antimalarials; Atovaquone; Cell Survival; Cytogenetics; DNA Damage; Dose-Response Relationship, Drug; Drug Combinations; Glutathione; Humans; Lymphocytes; Malaria, Falciparum; Male; Malondialdehyde; Oxidative Stress; Plasmodium falciparum; Proguanil; Triazines | 2015 |
Adaptive Landscape by Environment Interactions Dictate Evolutionary Dynamics in Models of Drug Resistance.
Topics: Antimalarials; Computational Biology; Drug Resistance; Evolution, Molecular; Humans; Inhibitory Concentration 50; Malaria, Falciparum; Models, Biological; Mutation; Plasmodium falciparum; Proguanil; Pyrimethamine; Triazines | 2016 |
In Vitro Analysis of the Interaction between Atovaquone and Proguanil against Liver Stage Malaria Parasites.
Topics: Antimalarials; Atovaquone; Drug Combinations; Hepatocytes; Humans; Inhibitory Concentration 50; Liver; Malaria, Falciparum; Plasmodium falciparum; Proguanil; Triazines | 2016 |
Adaptation of the [3H]Hypoxanthine Uptake Assay for In Vitro-Cultured Plasmodium knowlesi Malaria Parasites.
Topics: Animals; Antimalarials; Chloroquine; Clindamycin; Hypoxanthine; Inhibitory Concentration 50; Malaria; Plasmodium falciparum; Plasmodium knowlesi; Proguanil; Triazines | 2016 |
Herbicidal properties of antimalarial drugs.
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.
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 |
Proguanil and cycloguanil are organic cation transporter and multidrug and toxin extrusion substrates.
Topics: Antimalarials; HEK293 Cells; Humans; Octamer Transcription Factor-1; Organic Cation Transport Proteins; Organic Cation Transporter 2; Proguanil; Triazines | 2017 |
Characterization of Plasmodium knowlesi dihydrofolate reductase-thymidylate synthase and sensitivity to antifolates.
Topics: Antimalarials; Base Sequence; Folic Acid Antagonists; Multienzyme Complexes; Plasmodium knowlesi; Proguanil; Protozoan Proteins; Pyrimethamine; Sequence Alignment; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Triazines | 2018 |
Application of molecular docking and PSO-SVR intelligent approaches in antimalarial activity prediction of enantiomeric cycloguanil analogues.
Topics: Algorithms; Antimalarials; Enzyme Inhibitors; Folic Acid Antagonists; Machine Learning; Molecular Docking Simulation; Molecular Structure; Plasmodium falciparum; Proguanil; Protein Binding; Quantitative Structure-Activity Relationship; Reproducibility of Results; Stereoisomerism; Substrate Specificity; Tetrahydrofolate Dehydrogenase; Triazines | 2018 |
Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation.
Topics: Amides; Animals; Axons; Disease Models, Animal; Encephalitis; Encephalomyelitis, Autoimmune, Experimental; Female; Fluorescent Antibody Technique; Glaucoma; Male; Mice; Mice, Inbred C57BL; Myelin Sheath; Neuroprotective Agents; Optic Nerve; Peptoids; Proguanil; Pyrrolidinones; Rats; Rats, Sprague-Dawley; Real-Time Polymerase Chain Reaction; Triazines | 2019 |
Structural Insights into the Development of Cycloguanil Derivatives as
Topics: Enzyme Inhibitors; Hydrophobic and Hydrophilic Interactions; Models, Molecular; Molecular Structure; Oxidoreductases; Proguanil; Protozoan Proteins; Small Molecule Libraries; Structure-Activity Relationship; Triazines; Trypanocidal Agents; Trypanosoma brucei brucei | 2019 |
Cyclization-blocked proguanil as a strategy to improve the antimalarial activity of atovaquone.
Topics: Animals; Anopheles; Antimalarials; Atovaquone; Cyclization; Dihydroorotate Dehydrogenase; Dose-Response Relationship, Drug; Drug Combinations; Electron Transport Complex III; Enzyme Inhibitors; Erythrocytes; Folic Acid; Hep G2 Cells; Humans; Inhibitory Concentration 50; Liver; Oxidoreductases Acting on CH-CH Group Donors; Plasmodium berghei; Plasmodium falciparum; Proguanil; Sporozoites; Terpenes; Triazines | 2019 |
Discovery of new non-pyrimidine scaffolds as
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 |