Discovery of new non-pyrimidine scaffolds as <i>Plasmodium falciparum</i> DHFR inhibitors by fragment-based screening.

Hoarau, Marie; Vanichtanankul, Jarunee; Srimongkolpithak, Nitipol; Vitsupakorn, Danoo; Yuthavong, Yongyuth; Kamchonwongpaisan, Sumalee

Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening.

Hoarau, Marie; Vanichtanankul, Jarunee; Srimongkolpithak, Nitipol; Vitsupakorn, Danoo; Yuthavong, Yongyuth; Kamchonwongpaisan, Sumalee.

Afiliación

Hoarau M; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Vanichtanankul J; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Srimongkolpithak N; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Vitsupakorn D; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Yuthavong Y; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.
Kamchonwongpaisan S; National Center for Genetic Engineering and Biotechnology (BIOTEC), National Science and Technology Development Agency, Pathumthani, Thailand.

J Enzyme Inhib Med Chem ; 36(1): 198-206, 2021 Dec.

Article en En | MEDLINE | ID: mdl-33530764

Asunto(s)

Antimaláricos/farmacología; Descubrimiento de Drogas; Inhibidores Enzimáticos/farmacología; Plasmodium falciparum/efectos de los fármacos; Proteínas Protozoarias/antagonistas & inhibidores; Antimaláricos/síntesis química; Antimaláricos/química; Cristalografía por Rayos X; Relación Dosis-Respuesta a Droga; Evaluación Preclínica de Medicamentos; Inhibidores Enzimáticos/síntesis química; Inhibidores Enzimáticos/química; Modelos Moleculares; Simulación del Acoplamiento Molecular; Estructura Molecular; Plasmodium falciparum/enzimología; Proguanil/síntesis química; Proguanil/química; Proguanil/farmacología; Proteínas Protozoarias/aislamiento & purificación; Proteínas Protozoarias/metabolismo; Pirimetamina/síntesis química; Pirimetamina/química; Pirimetamina/farmacología; Relación Estructura-Actividad; Tetrahidrofolato Deshidrogenasa/aislamiento & purificación; Tetrahidrofolato Deshidrogenasa/metabolismo; Triazinas/síntesis química; Triazinas/química; Triazinas/farmacología

Palabras clave

Plasmodium falciparum; Malaria; dihydrofolate reductase; fragment-based screening; small molecule inhibitors

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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Plasmodium falciparum / Proteínas Protozoarias / Inhibidores Enzimáticos / Descubrimiento de Drogas / Antimaláricos Tipo de estudio: Diagnostic_studies / Screening_studies Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2021 Tipo del documento: Article País de afiliación: Tailandia

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