Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials | Zendy

Mariëtte van der Watt | Zendy; Janette Reader | Zendy; Alisje Churchyard | Zendy; Sindisiwe H. daba | Zendy; Sonja B. Lauterbach | Zendy; Jandeli Niemand | Zendy; Sijuade Abayomi | Zendy; Riëtte van Biljon | Zendy; Jessica Connacher | Zendy; Roelof van Wyk | Zendy; Claire Le Manach | Zendy; Tanya Paquet | Zendy; Diego Gonzàlez Cabrera | Zendy; Christel Brunschwig | Zendy; Anjo Theron | Zendy; Sonia Lozano-Arias | Zendy; Janneth Rodrigues | Zendy; Esperanza Herreros | Zendy; Didier Leroy | Zendy; James Duffy | Zendy; Leslie J. Street | Zendy; Kelly Chibale | Zendy; Dalu Mancama | Zendy; Thérèsa L. Coetzer | Zendy; LynMarié Birkholtz | Zendy

Open Access

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

Author(s) -

Mariëtte van der Watt,

Janette Reader,

Alisje Churchyard,

Sindisiwe H. daba,

Sonja B. Lauterbach,

Jandeli Niemand,

Sijuade Abayomi,

Riëtte van Biljon,

Jessica Connacher,

Roelof van Wyk,

Claire Le Manach,

Tanya Paquet,

Diego Gonzàlez Cabrera,

Christel Brunschwig,

Anjo Theron,

Sonia Lozano-Arias,

Janneth Rodrigues,

Esperanza Herreros,

Didier Leroy,

James Duffy,

Leslie J. Street,

Kelly Chibale,

Dalu Mancama,

Thérèsa L. Coetzer,

LynMarié Birkholtz

Publication year - 2018

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dky008

Subject(s) - gametocyte , plasmodium falciparum , biology , in silico , kinase , malaria , phenotypic screening , computational biology , microbiology and biotechnology , biochemistry , phenotype , immunology , gene

Novel chemical tools to eliminate malaria should ideally target both the asexual parasites and transmissible gametocytes. Several imidazopyridazines (IMPs) and 2-aminopyridines (2-APs) have been described as potent antimalarial candidates targeting lipid kinases. However, these have not been extensively explored for stage-specific inhibition of gametocytes in Plasmodium falciparum parasites. Here we provide an in-depth evaluation of the gametocytocidal activity of compounds from these chemotypes and identify novel starting points for dual-acting antimalarials.

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