ACS Medicinal Chemistry Letters
Letter
A.; MacDonald, S. J. F.; Santos Martínez, M.; Sanz, L. M.; Gamo, F. J.;
Fernandez, E. Cyclopropyl Carboxamides: A New Oral Antimalarial
Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).
ACS Med. Chem. Lett. 2011, 2, 840−844.
Present Addresses
§Ferrer R&D Center C, Juan de Sada, 32, E-08028
Barcelona, Spain.
∥School of Chemistry, University of Edinburgh, Joseph Black
Building, King's Buildings West Mains Road, Edinburgh, EH9
3JJ, United Kingdom.
́
(10) Sanz, L. M..; Jimenez-Díaz, M. B.; Crespo, B.; De-Cozar, C.;
Almela, M. J.; Angulo-Barturen, I.; Castaneda, P.; Ibanez, J.;
̃
̃
́
Fernandez, E.; Ferrer, S.; Herreros, E.; Lozano, S.; Martínez, M. S.;
Rueda, L.; Burrows, J. N.; García-Bustos, J. F.; Gamo, F. J. Cyclopropyl
Carboxamides, a Chemically Novel Class of Antimalarial Agents
Identified in a Phenotypic Screen. Antimicrob. Agents Chemother. 2011,
55, 5740−5745.
Author Contributions
The manuscript was written through contributions of all
authors. All authors have given approval to the final version of
the manuscript.
(11) Kessl, J. J.; Lange, B. B.; Merbitz-Zahradnik, T.; Zwicker, K.;
Funding
́
Hill, P.; Meunier, B.; Palsdottir, H.; Hunte, C.; Meshnick, S.;
GlaxoSmithKline acknowledges financial support from Medi-
cines for Malaria Venture (MMV).
Trumpower, B. Molecular Basis for Atovaquone Binding to the
Cytochrome bc1 Complex. J. Biol. Chem. 2003, 278, 31312−31318.
(12) See the Supporting Information.
Notes
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(16) Bromidge, S. M.; Dabbs, S.; Davies, D. T.; Malcolm Duckworth,
D.; Forbes, I. T.; Ham, P.; Jones, G. E.; King, F. D.; Saunders, D. V.;
Starr, S.; Thewlis, K. M.; Wyman, P. A.; Blaney, F. E.; Naylor, C. B.;
Bailey, F.; Blackburn, T. P.; Holland, V.; Kennett, G. A.; Riley, G. J.;
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The authors declare no competing financial interest.
ACKNOWLEDGMENTS
■
We thank our colleagues from the Computational, Analytical
and Structural Chemistry (CASC) department for the
measurement of the physicochemical properties of compounds
described in this paper, GSK Screening R&D group for the 5-
HT2c assays, Steve Bromidge for his contribution in the
understanding of the previous work carried out with the
indolines, the Cell Biology Group for the in vitro toxicity
studies, and Timothy J. Miles for his useful help.
(17) Bromidge, S. M.; Dabbs, S.; Davies, D. T.; Davies, S.; Malcolm
Duckworth, D.; Forbes, I. T.; Gaster, L. M.; Ham, P.; Jones, G. E.;
King, King, F. D.; Mulholland, K. R.; Saunders, D. V.; Wyman, P. A.;
Blaney, F. E.; Clarke, S. E.; Blackburn, T. P.; Holland, V.; Kennett, G.
A.; Lightowler, S.; Middlemiss, D. N.; Trail, B.; Riley, G.; Wood, M. D.
J. Med. Chem. 2000, 43, 1123−1134.
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