Table 2.
No. | Target | Scaffold | SAR plan from hit | Most advanced analogue | In vivo efficacy | Ref. |
---|---|---|---|---|---|---|
1.1 | InhA | Tetrahydro benzothieno pyrimidines |
N/Da | (Vilcheze et al., 2011) | ||
1.2 | L-Prolinamides | Nob | (Encinas et al., 2014) | |||
1.3 | Thiadiazolyl methylthiazoles | Yesc | (Sink et al., 2015) | |||
1.4 | 4-Hydroxy-2-pyridones | Yes | (Manjunatha et al., 2015; Ng et al., 2015) | |||
1.5 | Tetrahydropyranyl methylbenzamides | N/D | (Pajk et al., 2016) | |||
2.1 | KasA | Indazole sulfonamides | Yes | (Kumar et al., 2018; Cunningham et al., 2020) | ||
3.1 | Pks13 | Benzofurans | Yes | (Ioerger et al., 2013; Aggarwal et al., 2017) |
aN/D, not determined; bNo, inactive in an acute TB infection mouse model; cYes, active in an acute TB infection mouse model.