Table 1.
No. | Target | Scaffold | SAR plan from hit | Most advanced analogue | In vivo efficacy | Ref. |
---|---|---|---|---|---|---|
1.1 | DprE1 | 4−Aminoquinolone piperidine amides | N/Da | (Naik et al., 2014) | ||
1.2 | Pyrazolopyridones | N/D | (Panda et al., 2014) | |||
1.3 | 2-Carboxy quinoxalines |
N/D | (Neres et al., 2015) | |||
1.4 | 5-Hydroxy pyrimidinediones | N/D | (Oh et al., 2018) | |||
2.1 | MmpL3 | Adamantyl ureas | N/D | (Brown et al., 2011; North et al., 2013) | ||
2.2 | Indolecarboxamides | Yesb | (Onajole et al., 2013; Stec et al., 2016) | |||
2.3 | Yesb | (Kondreddi et al., 2013) | ||||
2.4 | Tetrahydropyrazolo pyrimidine carboxamide |
Yesb | (Remuinan et al., 2013; Yokokawa et al., 2013) | |||
2.5 | Spirocycles | Yesb | (Remuinan et al., 2013; Guardia et al., 2018) | |||
3.1 | MurI | Benzoxazoles | Yesc | (Malapati et al., 2018) |
aN/D, not determined; bYes, active in an acute TB infection mouse model; c Yes, active in Mycobacterium marinum infected adult zebrafish model.