Phosphonodiamidate prodrugs of N-alkoxy analogs of a fosmidomycin surrogate as antimalarial and antitubercular agents.

Courtens, Charlotte; Risseeuw, Martijn; Caljon, Guy; Cos, Paul; Martin, Anandi; Van Calenbergh, Serge

doi:10.1016/j.bmcl.2019.03.008

Phosphonodiamidate prodrugs of N-alkoxy analogs of a fosmidomycin surrogate as antimalarial and antitubercular agents.

Courtens, Charlotte

;

Risseeuw, Martijn

;

Caljon, Guy

;

Cos, Paul

;

Van Calenbergh, Serge

;et.al.

(2019) Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology — Vol. 29, n° 9, p. 1051-1053 (2019)

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Authors

Courtens, Charlotte
Author
Risseeuw, Martijn
Author
Caljon, Guy
Author
Cos, Paul
Author
Martin, AnandiUCLouvain
Author
Van Calenbergh, Serge
Author

Abstract

A series of N-alkoxy analogs of a l-leucine ethyl ester phosphonodiamidate prodrug of a fosmidomycin surrogate were synthesized and investigated for their ability to inhibit in vitro growth of P. falciparum and M. tuberculosis. These compounds originate by merging a previously reported successful phosphonate derivatisation with favorable modifications of the hydroxamate moiety. None of the synthesized compounds showed enhanced activity against either P. falciparum or M. tuberculosis in comparison with the parent free hydroxamate analog.

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Courtens, C., Risseeuw, M., Caljon, G., Cos, P., Martin, A., & Van Calenbergh, S. (2019). Phosphonodiamidate prodrugs of N-alkoxy analogs of a fosmidomycin surrogate as antimalarial and antitubercular agents. Bioorganic & Medicinal Chemistry Letters : the tetrahedron journal for research at the interface of chemistry and biology, 29(9), 1051-1053. https://doi.org/10.1016/j.bmcl.2019.03.008 (Original work published 2019)