Optimization of diastereomeric dihydropyridines as antimalarials

Autor: Van Horn, Kurt S., Zhao, Yingzhao, Parvatkar, Prakash T., Maier, Julie, Mutka, Tina, Lacrue, Alexis, Brockmeier, Fabian, Ebert, Daniel, Wu, Wesley, Casandra, Debora R., Namelikonda, Niranjan, Yacoub, Jeanine, Sigal, Martina, Knapp, Spencer, Floyd, David, Waterson, David, Burrows, Jeremy N., Duffy, James, DeRisi, Joseph L., Kyle, Dennis E., Guy, R. Kiplin, Manetsch, Roman

Publikováno v: In European Journal of Medicinal Chemistry 5 September 2024 275

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Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity

Autor: Kokkonda, Sreekanth, El Mazouni, Farah, White, Karen L, White, John, Shackleford, David M, Lafuente-Monasterio, Maria Jose, Rowland, Paul, Manjalanagara, Krishne, Joseph, Jayan T, Garcia-Pérez, Adolfo, Fernandez, Jorge, Gamo, Francisco Javier, Waterson, David, Burrows, Jeremy N, Palmer, Michael J, Charman, Susan A, Rathod, Pradipsinh K, Phillips, Margaret A

Publikováno v: Repositorio Institucional de la Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid

Malaria kills nearly 0.5 million people yearly and impacts the lives of those living in over 90 countries where it is endemic. The current treatment programs are threatened by increasing drug resistance. Dihydroorotate dehydrogenase (DHODH) is now cl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=RECOLECTA___::2c029d74f816d92febe7eba4eb3d3c56
https://repositoriosaludmadrid.es/handle/20.500.12530/35603

MOESM1 of Screening a protein kinase inhibitor library against Plasmodium falciparum

Autor: Hallyburton, Irene, Grimaldi, Raffaella, Woodland, Andrew, BaragaĂąa, Beatriz, Luksch, Torsten, Spinks, Daniel, James, Daniel, Leroy, Didier, Waterson, David, Fairlamb, Alan, Wyatt, Paul, Gilbert, Ian, Frearson, Julie

Additional file 1. Supplementary information.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::057319f1826cc16fbbcad21be5d0bfab

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

Autor: Norcross, Neil R., Baragaña, Beatriz, Wilson, Caroline, Hallyburton, Irene, Osuna-Cabello, Maria, Norval, Suzanne, Riley, Jennifer, Stojanovski, Laste, Simeons, Frederick R. C., Porzelle, Achim, Grimaldi, Raffaella, Wittlin, Sergio, Duffy, Sandra, Avery, Vicky M., Meister, Stephan, Sanz, Laura, Jiménez-Díaz, Belén, Angulo-Barturen, Iñigo, Ferrer, Santiago, Martínez, María Santos, Gamo, Francisco Javier, Frearson, Julie A., Gray, David W., Fairlamb, Alan H., Winzeler, Elizabeth A., Waterson, David, Campbell, Simon F., Willis, Paul, Read, Kevin D., Gilbert, Ian H.

Publikováno v: Repositorio Institucional de la Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid
Journal of Medicinal Chemistry

In this paper we describe the optimization of a phenotypic hit against Plasmodium falciparum, based on a trisubstituted pyrimidine scaffold. This led to compounds with good pharmacokinetics and oral activity in a P. berghei mouse model of malaria. Th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::a62735feb2ed620d248ceef35a49e034
https://repositoriosaludmadrid.es/handle/20.500.12530/26152