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Relevant bibliographies by topics / Cycloguanil

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Academic literature on the topic 'Cycloguanil'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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Journal articles on the topic "Cycloguanil"

1

Brown, Jennifer I., Peng Wang, Alan Y. L. Wong, et al. "Cycloguanil and Analogues Potently Target DHFR in Cancer Cells to Elicit Anti-Cancer Activity." Metabolites 13, no. 2 (2023): 151. http://dx.doi.org/10.3390/metabo13020151.

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Dihydrofolate reductase (DHFR) is an established anti-cancer drug target whose inhibition disrupts folate metabolism and STAT3-dependent gene expression. Cycloguanil was proposed as a DHFR inhibitor in the 1950s and is the active metabolite of clinically approved plasmodium DHFR inhibitor Proguanil. The Cycloguanil scaffold was explored to generate potential cancer therapies in the 1970s. Herein, current computational and chemical biology techniques were employed to re-investigate the anti-cancer activity of Cycloguanil and related compounds. In silico modeling was employed to identify promisi

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2

Edstein, M. D., S. Bahr, B. Kotecka, G. D. Shanks, and K. H. Rieckmann. "In vitro activities of the biguanide PS-15 and its metabolite, WR99210, against cycloguanil-resistant Plasmodium falciparum isolates from Thailand." Antimicrobial Agents and Chemotherapy 41, no. 10 (1997): 2300–2301. http://dx.doi.org/10.1128/aac.41.10.2300.

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The in vitro activities of the new biguanide PS-15 and its putative active metabolite, WR99210, were determined against seven different isolates or clones of Plasmodium falciparum. The mean 50% inhibitory concentrations of PS-15 and WR99210 were 1,015 and 0.06 ng/ml, respectively. WR99210 was up to 363 times more potent than cycloguanil, the active metabolite of proguanil, against cycloguanil-resistant parasites. The pronounced activity of WR99210 against multidrug-resistant P. falciparum indicates that further studies are required to determine the value of the prodrug, PS-15, as an antimalari

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3

Zhigulin, Arseniy S., Anastasiya O. Novikova, and Oleg I. Barygin. "Mechanisms of NMDA Receptor Inhibition by Biguanide Compounds." Pharmaceuticals 17, no. 9 (2024): 1234. http://dx.doi.org/10.3390/ph17091234.

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N-methyl-D-aspartate (NMDA) receptors are inhibited by many medicinal drugs. The recent successful repurposing of NMDA receptor antagonists ketamine and dextromethorphan for the treatment of major depressive disorder further enhanced the interest in this field. In this work, we performed a screening for the activity against native NMDA receptors of rat CA1 hippocampal pyramidal neurons among biguanide compounds using the whole-cell patch-clamp method. Antimalarial biguanides proguanil and cycloguanil, as well as hypoglycemic biguanide phenformin, inhibited them in micromolar concentrations, wh

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Kurniawan, Isman, Muhammad Salman Fareza, and Ponco Iswanto. "CoMFA, Molecular Docking and Molecular Dynamics Studies on Cycloguanil Analogues as Potent Antimalarial Agents." Indonesian Journal of Chemistry 21, no. 1 (2020): 66. http://dx.doi.org/10.22146/ijc.52388.

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Malaria is a disease that commonly infects humans in many tropical areas. This disease becomes a serious problem because of the high resistance of Plasmodium parasite against the well-established antimalarial agents, such as Artemisinin. Hence, new potent compounds are urgently needed to resolve this resistance problem. In the present study, we investigated cycloguanil analogues as a potent antimalarial agent by utilizing several studies, i.e., comparative of molecular field analysis (CoMFA), molecular docking and molecular dynamics (MD) simulation. A CoMFA model with five partial least square

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5

Schwalbe, C. H., G. J. B. Williams, and T. F. Koetzle. "Structure of cycloguanil hydrochloride by neutron diffraction." Acta Crystallographica Section C Crystal Structure Communications 45, no. 3 (1989): 468–71. http://dx.doi.org/10.1107/s0108270188012193.

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6

Ralaimazava, P., R. Durand, N. Godineau, et al. "Profile and evolution of the chemosusceptibility of falciparum malaria imported into France in 2000." Eurosurveillance 7, no. 7 (2002): 113–18. http://dx.doi.org/10.2807/esm.07.07.00355-en.

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In 2000, the chemosusceptibility of imported malaria was stable in France. All countries of infection considered, the bi-resistance to chloroquine and cycloguanil has not changed from 1996 to 2000. The monotherapy using quinine or mefloquine remains the first-line treatment to falciparum malaria. Resistance to these two antimalarials is rare in Africa and has not evolved over the past 15 years.

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Pudney, Mary, Win Gutteridge, Anton Zeman, Maurice Dickins, and Joseph L. Woolley. "Atovaquone and Proguanil Hydrochloride: A Review of Nonclinical Studies." Journal of Travel Medicine 6, S1 (1999): S8—S12. http://dx.doi.org/10.1093/jtm/6.suppl.s8.

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Abstract Background: Safe and effective antimalarial drugs are needed for treatment and prophylaxis of malaria. The combination of atovaquone and proguanil hydrochloride is a new antimalarial drug combination that has recently become available in many countries. Methods: Data were reviewed from nonclinical studies evaluating the microbiology, secondary pharmacology, pharmacokinetics, and toxicology of atovaquone and proguanil hydrochloride. Results: Atovaquone is highly active against asexual erythrocytic stages of Plasmodium falciparum in vitro (IC60 0.7-6 nM) and in animal models. Proguanil

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8

Arnold, Megan S. J., Jessica A. Engel, Ming Jang Chua, Gillian M. Fisher, Tina S. Skinner-Adams, and Katherine T. Andrews. "Adaptation of the [3H]Hypoxanthine Uptake Assay forIn Vitro-Cultured Plasmodium knowlesi Malaria Parasites." Antimicrobial Agents and Chemotherapy 60, no. 7 (2016): 4361–63. http://dx.doi.org/10.1128/aac.02948-15.

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ABSTRACTThe zoonotic malaria parasitePlasmodium knowlesihas recently been established in continuousin vitroculture. Here, thePlasmodium falciparum[3H]hypoxanthine uptake assay was adapted forP. knowlesiand used to determine the sensitivity of this parasite to chloroquine, cycloguanil, and clindamycin. The data demonstrate thatP. knowlesiis sensitive to all drugs, with 50% inhibitory concentrations (IC50s) consistent with those obtained withP. falciparum. This assay provides a platform to useP. knowlesi in vitrofor drug discovery.

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Barata, Lídia, Pascal Houzé, Khadija Boutbibe, et al. "In VitroAnalysis of the Interaction between Atovaquone and Proguanil against Liver Stage Malaria Parasites." Antimicrobial Agents and Chemotherapy 60, no. 7 (2016): 4333–35. http://dx.doi.org/10.1128/aac.01685-15.

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ABSTRACTThe interaction between atovaquone and proguanil has never been studied against liver stage malaria, which is the main target of this drug combination when used for chemoprevention. Using human hepatocytes lacking cytochrome P450 activity, and thus avoiding proguanil metabolizing into potent cycloguanil, we showin vitrothat the atovaquone-proguanil combination synergistically inhibits the growth of rodentPlasmodium yoeliiparasites. These results provide a pharmacological basis for the high efficacy of atovaquone-proguanil used as malaria chemoprevention.

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10

Scott, H. V., M. D. Edstein, J. R. Veenendaal, and K. H. Rieckmann. "A sensitive bioassay for serum cycloguanil using Plasmodium falciparumin vitro." International Journal for Parasitology 18, no. 5 (1988): 605–9. http://dx.doi.org/10.1016/0020-7519(88)90094-x.

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Dissertations / Theses on the topic "Cycloguanil"

1

Tann, Annabelle. "Bedeutung genetischer Polymorphismen im organischen Kationentransporter OCT1 für die Pharmakokinetik und Nebenwirkungen von Proguanil." Doctoral thesis, 2019. http://hdl.handle.net/11858/00-1735-0000-002E-E564-A.

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Conference papers on the topic "Cycloguanil"

1

Hecht, David, Mars Cheung, and Gary B. Fogel. "Docking scores and QSAR using evolved neural networks for the Pan-inhibition of wild-type and mutant PfDHFR by cycloguanil derivatives." In 2009 IEEE Congress on Evolutionary Computation (CEC). IEEE, 2009. http://dx.doi.org/10.1109/cec.2009.4982957.

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