Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate

Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate

The widespread emergence of Plasmodium falciparum (Pf) strains resistant to frontline agents has fuelled the search for fast-acting agents with novel mechanism of action. Here, we report the discovery and optimization of novel antimalarial compounds, the triaminopyrimidines (TAPs), which emerged fro...

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Hauptverfasser: Hameed P., Shahul, Solapure, Suresh, Patil, Vikas, Henrich, Philipp P, Magistrado, Pamela A, Bharath, Sowmya, Murugan, Kannan, Viswanath, Pavithra, Puttur, Jayashree, Srivastava, Abhishek, Bellale, Eknath, Panduga, Vijender, Shanbag, Gajanan, Awasthy, Disha, Landge, Sudhir, Morayya, Sapna, Koushik, Krishna, Saralaya, Ramanatha, Raichurkar, Anandkumar, Rautela, Nikhil, Roy Choudhury, Nilanjana, Ambady, Anisha, Nandishaiah, Radha, Reddy, Jitendar, Prabhakar, K. R, Menasinakai, Sreenivasaiah, Rudrapatna, Suresh, Chatterji, Monalisa, Jiménez-Díaz, María Belén, Martínez, María Santos, Sanz, Laura María, Coburn-Flynn, Olivia, Fidock, David A, Lukens, Amanda K, Wirth, Dyann F, Bandodkar, Balachandra, Mukherjee, Kakoli, McLaughlin, Robert E, Waterson, David, Rosenbrier-Ribeiro, Lyn, Hickling, Kevin, Balasubramanian, V, Warner, Peter, Hosagrahara, Vinayak, Dudley, Adam, Iyer, Pravin S, Narayanan, Shridhar, Kavanagh, Stefan, Sambandamurthy, Vasan K
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Sprache:eng
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Zusammenfassung:The widespread emergence of Plasmodium falciparum (Pf) strains resistant to frontline agents has fuelled the search for fast-acting agents with novel mechanism of action. Here, we report the discovery and optimization of novel antimalarial compounds, the triaminopyrimidines (TAPs), which emerged from a phenotypic screen against the blood stages of Pf. The clinical candidate (compound 12) is efficacious in a mouse model of Pf malaria with an ED99
ISSN:2041-1723
2041-1723
DOI:10.1038/ncomms7715