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

Shahul Hameed P., Suresh Solapure, Vikas Patil, Philipp P. Henrich, Pamela A. Magistrado, Sowmya Bharath, Kannan Murugan, Pavithra Viswanath, Jayashree Puttur, Abhishek Srivastava, Eknath Bellale, Vijender Panduga, Gajanan Shanbag, Disha Awasthy, Sudhir Landge, Sapna Morayya, Krishna Koushik, Ramanatha Saralaya, Anandkumar Raichurkar, Nikhil Rautela, Nilanjana Roy Choudhury, Anisha Ambady, Radha Nandishaiah, Jitendar Reddy, K. R. Prabhakar, Sreenivasaiah Menasinakai, Suresh Rudrapatna, Monalisa Chatterji, María Belén Jiménez-Díaz, María Santos Martínez, Laura María Sanz, Olivia Coburn-Flynn, David A. Fidock, Amanda K. Lukens, Dyann F. Wirth, Balachandra Bandodkar, Kakoli Mukherjee, Robert E. McLaughlin, David Waterson, Lyn Rosenbrier-Ribeiro, Kevin Hickling, V. Balasubramanian, Peter Warner, Vinayak Hosagrahara, Adam Dudley, Pravin S. Iyer, Shridhar Narayanan, Stefan Kavanagh () and Vasan K. Sambandamurthy ()
Additional contact information
Shahul Hameed P.: AstraZeneca India Pvt. Ltd.
Suresh Solapure: AstraZeneca India Pvt. Ltd.
Vikas Patil: AstraZeneca India Pvt. Ltd.
Philipp P. Henrich: Columbia University Medical Center
Pamela A. Magistrado: Harvard School of Public Health
Sowmya Bharath: AstraZeneca India Pvt. Ltd.
Kannan Murugan: AstraZeneca India Pvt. Ltd.
Pavithra Viswanath: AstraZeneca India Pvt. Ltd.
Jayashree Puttur: AstraZeneca India Pvt. Ltd.
Abhishek Srivastava: AstraZeneca India Pvt. Ltd.
Eknath Bellale: AstraZeneca India Pvt. Ltd.
Vijender Panduga: AstraZeneca India Pvt. Ltd.
Gajanan Shanbag: AstraZeneca India Pvt. Ltd.
Disha Awasthy: AstraZeneca India Pvt. Ltd.
Sudhir Landge: AstraZeneca India Pvt. Ltd.
Sapna Morayya: AstraZeneca India Pvt. Ltd.
Krishna Koushik: AstraZeneca India Pvt. Ltd.
Ramanatha Saralaya: AstraZeneca India Pvt. Ltd.
Anandkumar Raichurkar: AstraZeneca India Pvt. Ltd.
Nikhil Rautela: AstraZeneca India Pvt. Ltd.
Nilanjana Roy Choudhury: AstraZeneca India Pvt. Ltd.
Anisha Ambady: AstraZeneca India Pvt. Ltd.
Radha Nandishaiah: AstraZeneca India Pvt. Ltd.
Jitendar Reddy: AstraZeneca India Pvt. Ltd.
K. R. Prabhakar: AstraZeneca India Pvt. Ltd.
Sreenivasaiah Menasinakai: AstraZeneca India Pvt. Ltd.
Suresh Rudrapatna: AstraZeneca India Pvt. Ltd.
Monalisa Chatterji: AstraZeneca India Pvt. Ltd.
María Belén Jiménez-Díaz: Tres Cantos Medicines Development Campus. Diseases of Developing World (DDW), GlaxoSmithKline
María Santos Martínez: Tres Cantos Medicines Development Campus. Diseases of Developing World (DDW), GlaxoSmithKline
Laura María Sanz: Tres Cantos Medicines Development Campus. Diseases of Developing World (DDW), GlaxoSmithKline
Olivia Coburn-Flynn: Columbia University Medical Center
David A. Fidock: Columbia University Medical Center
Amanda K. Lukens: Harvard School of Public Health
Dyann F. Wirth: Harvard School of Public Health
Balachandra Bandodkar: AstraZeneca India Pvt. Ltd.
Kakoli Mukherjee: AstraZeneca India Pvt. Ltd.
Robert E. McLaughlin: AstraZeneca Infection Innovative Medicines
David Waterson: Medicines for Malaria Venture, International Center Cointrin
Lyn Rosenbrier-Ribeiro: AstraZeneca
Kevin Hickling: AstraZeneca
V. Balasubramanian: AstraZeneca India Pvt. Ltd.
Peter Warner: AstraZeneca India Pvt. Ltd.
Vinayak Hosagrahara: AstraZeneca India Pvt. Ltd.
Adam Dudley: AstraZeneca India Pvt. Ltd.
Pravin S. Iyer: AstraZeneca India Pvt. Ltd.
Shridhar Narayanan: AstraZeneca India Pvt. Ltd.
Stefan Kavanagh: AstraZeneca
Vasan K. Sambandamurthy: AstraZeneca India Pvt. Ltd.

Nature Communications, 2015, vol. 6, issue 1, 1-11

Abstract: Abstract 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

Date: 2015
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DOI: 10.1038/ncomms7715

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