Inhibition of Leishmania mexicana Growth by the Tuberculosis Drug SQ109 | Zendy

Verónica A. García-García | Zendy; Eric Oldfield | Zendy; Gustavo Benaím | Zendy

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Inhibition of Leishmania mexicana Growth by the Tuberculosis Drug SQ109

Author(s) -

Verónica A. García-García,

Eric Oldfield,

Gustavo Benaím

Publication year - 2016

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00945-16

Subject(s) - leishmania mexicana , amastigote , leishmania , axenic , drug , protonophore , mycobacterium tuberculosis , chemistry , pharmacology , organelle , leishmaniasis , biochemistry , intracellular , biology , microbiology and biotechnology , tuberculosis , mitochondrion , immunology , medicine , parasite hosting , bacteria , pathology , world wide web , computer science , genetics

We report that the tuberculosis drug SQ109 [N -adamantan-2-yl-N ′-((E )-3,7-dimethyl-octa-2,6-dienyl)-ethane-1,2-diamine] has potent activity against the intracellular amastigote form ofLeishmania mexicana (50% inhibitory concentration [IC50 ], ∼11 nM), with a good selectivity index (>500). It is also active against promastigotes (IC50 , ∼500 nM) and acts as a protonophore uncoupler, in addition to disrupting Ca2+ homeostasis by releasing organelle Ca2+ into the cytoplasm, and as such, it is an interesting new leishmaniasis drug hit candidate.

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