Table 2.
Antitubercular agents inhibiting mycolic acid biosynthesis.
No. | Target | Scaffold | SAR plan from hit | Most advanced analogue | In vivo efficacy | Ref. |
---|---|---|---|---|---|---|
1.1 | InhA | Tetrahydro benzothieno pyrimidines |
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N/Da | (Vilcheze et al., 2011) |
1.2 | L-Prolinamides |
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Nob | (Encinas et al., 2014) | |
1.3 | Thiadiazolyl methylthiazoles |
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Yesc | (Sink et al., 2015) | |
1.4 | 4-Hydroxy-2-pyridones |
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Yes | (Manjunatha et al., 2015; Ng et al., 2015) | |
1.5 | Tetrahydropyranyl methylbenzamides |
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N/D | (Pajk et al., 2016) | |
2.1 | KasA | Indazole sulfonamides |
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Yes | (Kumar et al., 2018; Cunningham et al., 2020) |
3.1 | Pks13 | Benzofurans |
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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.