Abstract
Malaria is a leading cause of human death within the tropics. The gradual generation of drug resistance imposes an urgent need for the development of new and selective antimalarial agents. Kinetic isotope effects coupled to computational chemistry have provided the relevant details on geometry and charge of enzymatic transition states to facilitate the design of transition-state analogs. These features have been reproduced into chemically stable mimics through synthetic chemistry, generating inhibitors with dissociation constants in the pico- to femto-molar range. Transition-state analogs are expected to contribute to the control of malaria.
Original language | English (US) |
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Pages (from-to) | 1341-1360 |
Number of pages | 20 |
Journal | Future Medicinal Chemistry |
Volume | 5 |
Issue number | 11 |
DOIs | |
State | Published - Jul 2013 |
ASJC Scopus subject areas
- Molecular Medicine
- Pharmacology
- Drug Discovery