Table 3.
No. | Target | Scaffold | SAR plan from hit | Most advanced analogue | In vivo efficacy | Ref. |
---|---|---|---|---|---|---|
1.1 | NDH-2 | Quinolinyl pyrimidines | N/Da | (Shirude et al., 2012) | ||
1.2 | Quinolones | N/D | (Hong et al., 2017) | |||
1.3 | 2−Mercapto quinazolinones |
N/D | (Murugesan et al., 2018) | |||
1.4 | N/D | (Harbut et al., 2018) | ||||
2.1 | QcrB | Alkyl benzimidazoles | N/D | (Chandrasekera et al., 2015; Chandrasekera et al., 2017) | ||
2.2 | Morpholino thiophenes |
Yesb | (Cleghorn et al., 2018) | |||
3.1 | MenG | Biphenyl amides | N/D | (Sukheja et al., 2017) |
aN/D, not determined; bYes, active in an acute TB infection mouse model.