Yongyuth Yuthavong

Identification of vulnerable antimalarial targets using conditional loss of function mutants

Philip J. Shaw, Parichat Prommana, Chayaphat Wongsombat, Jutharat Pengon et autres

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Repurpose antimalarials to target Toxoplasma gondii dihydrofolate reductase thymidylate synthase

Sasithorn Decharuangsilp, Khuanchai N. Koompapong, Uthai Arwon, Nongnaput Tuyapala et autres

Toxoplasma gondii is an obligate intracellular blood and tissue protozoan parasite that infects up to a third of the population worldwide. Several antimalarial drugs, in particular pyrimethamine ( PYR ), have been used for decades to treat toxoplasmosis. Here, the clinical Pf …

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Lipophilic Pyrimethamine analogs with anti-toxoplasmosis activity

Darin Kongkasuriyachai, Khuanchai N. Koompapong, Nongnaput Tuyapala, Marie Hoarau et autres

Toxoplasmosis remains a threat for neonates and immuno-compromised populations, against which only broad spectrum antiparasitic drugs are currently available. Here, a virtual screen was conducted on a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor library to identify novel Toxoplasma gondii DHFR inhibitors. Three …

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ScienceAsia reflects the maturity of science in Thailand and Asia

Yongyuth Yuthavong

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Antifolate Drugs

Yongyuth Yuthavong

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Flexible 2,4-diaminopyrimidine bearing a butyrolactone as Plasmodium falciparum dihydrofolate reductase inhibitors

Sasithorn Decharuangsilp, Uthai Arwon, Marie Hoarau, Jarunee Vanichtanankul et autres

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folA thyA knockout E. coli as a suitable surrogate model for evaluation of antifolate sensitivity against PfDHFR-TS

Nattida Suwanakitti, Yuwadee Talawanich, Jarunee Vanichtanankul, Supannee Taweechai et autres

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Novel flexible biphenyl Pf DHFR inhibitors with improved antimalarial activity

Sasithorn Decharuangsilp, Uthai Arwon, Nawarat Sooksai, Roonglawan Rattanajak et autres

and suitable drug-like properties. This confirms the importance of compound flexibility for antimalarial activity and opens the way to new opportunities for antimalarial drug design.

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Flexible 2,4-Diaminopyrimidine Bearing a Butyrolactone as Plasmodium Falciparum Dihydrofolate Reductase Inhibitors

Sasithorn Decharuangsilp, Uthai Arwon, Marie Hoarau, Jarunee Vanichtanankul et autres

Nigéria, th (code pays fourni par la source)

Fola Thya Knockout E. Coli as a Suitable Surrogate Model for Evaluation of Antifolate Sensitivity Against Pfdhfr-Ts

Nattida Suwanakitti, Yuwadee Talawanich, Jarunee Vanichtanankul, Supannee Taweechai et autres

Nigéria, th (code pays fourni par la source)

Development of a Practical Synthetic Method for Clinical Candidate 3-(2-{3-[(2,4-Diamino-6-ethylpyrimidin-5-yl)oxy]propoxy} phenyl)propanoic acid (P218) and Its Hydroxylated Metabolites

Nitipol Srimongkolpithak, Onanong Vorasin, Tanawat Phumjan, Siriporn Saepua et autres

Abstract 3-(2-{3-[(2,4-Diamino-6-ethylpyrimidin-5-yl)oxy]propoxy}phenyl)propanoic acid, known as P218, has demonstrated great potency and safety in preclinical and human studies. However, the previous synthetic methods for P218 gave low yields and required hazardous reagents and challenging procedures. In this study, we have successfully developed a …

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Susceptibility of Southeast Asian Plasmodium falciparum isolates to P218

Navaporn Posayapisit, Jutharat Pengon, Philip James Shaw, Chairat Uthaipibull et autres

A major threat to the goal of eliminating malaria, particularly in Southeast Asia, is the spread of Plasmodium falciparum resistant to artemisinin-based combination therapies. P218 is a drug candidate designed to combat antifolate-sensitive and -resistant parasites. However, there is no evidence that …

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