Figure 1: The anti-tubercular activity of GSK3011724A.
From: Identification of KasA as the cellular target of an anti-tubercular scaffold
(a) Chemical structure of GSK3011724A. (b,c) GSK3011724A was evaluated in an acute (b) and chronic (c) model of murine TB infection. Each symbol represents data from a single mouse. A two-fold log c.f.u. reduction equates to a 2 log c.f.u. difference compared with untreated mice at the end of the treatment period. Untreated mice gave a log c.f.u. count of 7.1±0.1 (mean±s.d., n=5 mice) in the acute assay and 5.8±0.26 (mean±s.d., n=7 mice for the INH experiment) or 6.0±0.5 (mean±s.d., n=5 mice for GSK3011724A experiment) in the chronic assay. (d) Comparison of the in vivo efficacy of GSK3011724A and INH against M. tuberculosis H37Rv wild-type (H37Rv WT) and M. tuberculosis KasA mutant strains. Mice were infected with each strain and administered with INH or GSK3011724A at different doses during the acute phase (days 1 to 8 after infection). Each dot represents data from a single mouse. Log c.f.u. counts are shown as the difference with respect to the untreated group infected with each strain (Δlog c.f.u. for each mouse).
