Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential

Jose Coteron, Maria Marco, Jorge Esquivias, Xiaoyi Deng, Karen White, John White, Maria Koltun, Farah El Mazouni, Sreekanth Kokkonda, Kasiram Katneni, Ravi Bhamidipati, David Shackleford, Inigo Angulo-Barturen, Santiago Ferrer, Maria Belen Jimenez-Diaz, Francisco-Javier Gamo, Elizabeth Goldsmith, William Charman, Ian Bathurst, David FloydDavid Matthews, Jeremy Burrows, Pradip Rathod, Susan Charman, Margaret Phillips

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Abstract

Drug therapy is the mainstay of antimalarial therapy, yet current drugs are threatened by the development of resistance. In an effort to identify new potential antimalarials, we have undertaken a lead optimization program around our previously identified triazolopyrimidine-based series of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors.
Original languageEnglish
Pages (from-to)5540 - 5561
Number of pages22
JournalJournal of Medicinal Chemistry
Volume54
Issue number15
DOIs
Publication statusPublished - 2011

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