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Potent antimalarials with development potential identified by structure-guided computational optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series

Dihydroorotate dehydrogenase (DHODH) has been clinically validated as a target for the development of new antimalarials. Experience with clinical candidate triazolopyrimidine DSM265 (1) suggested that DHODH inhibitors have great potential for use in prophylaxis, which represents an unmet need in the...

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Publicat a:J Med Chem
Autors principals: Palmer, Michael J., Deng, Xiaoyi, Watts, Shawn, Krilov, Goran, Gerasyuto, Aleksey, Kokkonda, Sreekanth, El Mazouni, Farah, White, John, White, Karen L., Striepen, Josefine, Bath, Jade, Schindler, Kyra, Yeo, Tomas, Shackleford, David M., Mok, Sachel, Deni, Ioanna, Lawong, Aloysus, Huang, Ann, Chen, Gong, Wang, Wen, Jayaseelan, Jaya, Katneni, Kasiram, Patil, Rahul, Saunders, Jessica, Shahi, Shatrughan P., Chittimalla, Rajesh, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Wittlin, Sergio, Tumwebaze, Patrick K., Rosenthal, Philip J., Cooper, Roland A., Campos Aguiar, Anna Caroline, Guido, Rafael V.C., Pereira, Dhelio B., Mittal, Nimisha, Winzeler, Elizabeth A., Tomchick, Diana R., Laleu, Benoît, Burrows, Jeremy N., Rathod, Pradipsinh K., Fidock, David A., Charman, Susan A., Phillips, Margaret A.
Format: Artigo
Idioma:Inglês
Publicat: 2021
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC8171248/
https://ncbi.nlm.nih.gov/pubmed/33876936
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.1c00173
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