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. 2021 Mar 15;11:611304. doi: 10.3389/fcimb.2021.611304

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
graphic file with name fcimb-11-611304-g021.jpg graphic file with name fcimb-11-611304-g022.jpg N/Da (Vilcheze et al., 2011)
1.2 L-Prolinamides graphic file with name fcimb-11-611304-g023.jpg graphic file with name fcimb-11-611304-g024.jpg Nob (Encinas et al., 2014)
1.3 Thiadiazolyl methylthiazoles graphic file with name fcimb-11-611304-g025.jpg graphic file with name fcimb-11-611304-g026.jpg Yesc (Sink et al., 2015)
1.4 4-Hydroxy-2-pyridones graphic file with name fcimb-11-611304-g027.jpg graphic file with name fcimb-11-611304-g028.jpg Yes (Manjunatha et al., 2015; Ng et al., 2015)
1.5 Tetrahydropyranyl methylbenzamides graphic file with name fcimb-11-611304-g029.jpg graphic file with name fcimb-11-611304-g030.jpg N/D (Pajk et al., 2016)
2.1 KasA Indazole sulfonamides graphic file with name fcimb-11-611304-g031.jpg graphic file with name fcimb-11-611304-g032.jpg Yes (Kumar et al., 2018; Cunningham et al., 2020)
3.1 Pks13 Benzofurans graphic file with name fcimb-11-611304-g033.jpg graphic file with name fcimb-11-611304-g034.jpg 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.