Table 4.
No. | Target | Scaffold | SAR plan from hit | Most advanced analogue | In vivo efficacy | Ref. |
---|---|---|---|---|---|---|
1.1 | Rv0577 | Pyrimidine imidazoles | Noa | (Pethe et al., 2010) | ||
2.1 | FtsZ | Benzimidazoles | N/Db | (Kumar et al., 2011; Awasthi et al., 2013) | ||
3.1 | EthR | N-phenylphenoxy acetamides | N/D | (Flipo et al., 2012) | ||
4.1 | LepB | Arylhydrazones | N/D | (Bonnett et al., 2016) | ||
5.1 | CysM | Diphenyl ureas | N/D | (Brunner et al., 2016) | ||
6.1 | BioA | Benzoyl piperazines |
N/D | (Park et al., 2015; Liu et al., 2017) | ||
7.1 | IMPDH | Indazole sulfonamides | No | (Park et al., 2017) | ||
7.2 | Benzoxazoles | N/D | (Chacko et al., 2018) | |||
8.1 | PknA PknB |
Pyrazolyl pyrimidinamine |
N/D | (Wang et al., 2017) | ||
9.1 | CorA | Pyrimidinetrione amides |
No | (Park et al., 2019) | ||
10.1 | DosS DosT |
Ureas | N/D | (Zheng et al., 2020) |
aNo, inactive in an acute TB infection mouse model; bN/D, not determined.