Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

Nobutaka Kato,Eamon Comer,Tomoyo Sakata-Kato,Arvind Sharma,Manmohan Sharma,Micah Maetani,Jessica Bastien,Nicolas M. B. Brancucci,Joshua A. Bittker,Victoria C. Corey,David J. Clarke,Emily R. Derbyshire,Gillian L. Dornan,Sandra Duffy,Sean Eckley,Maurice A. Itoe,Karin M. J. Koolen,Timothy A. Lewis,Ping S. Lui,Amanda K Lukens,Emily Lund,Sandra March,Elamaran Meibalan,Bennett C. Meier,Jacob A. McPhail,Branko Mitasev,Eli L. Moss,Morgane Sayes,Yvonne Van Gessel,Mathias J. Wawer,Takashi Yoshinaga,Anne-Marie Zeeman,Vicky M. Avery,Sangeeta N. Bhatia,John E. Burke,Flaminia Catteruccia,Jon Clardy,Paul A. Clemons,Koen J. Dechering,Jeremy R. Duvall,Michael A. Foley,Fabian Gusovsky,Clemens H. M. Kocken,Matthias Marti,Marshall L. Morningstar,Benito Munoz,Daniel E. Neafsey,Amit Sharma,Elizabeth A. Winzeler,Dyann F. Wirth,Christina Scherer,Stuart L. Schreiber

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors

2016

The bicyclic azetidines, a class of potent, well-tolerated antimalarial compounds that is active against multiple stages of the Plasmodium life-cycle, has been discovered following screens against libraries of compounds reminiscent of natural products.

Keywords:

Combinatorial chemistry
Phenylalanine—tRNA ligase
Small molecule
Biochemistry
Drug discovery
Parasitology
Phenylurea Compounds
Bicyclic molecule
Azabicyclo Compounds
Chemistry
Plasmodium falciparum
Humanized mouse
Antimalarial Agent
Malaria
Biology
Computational biology

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