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

Table 1.

Antitubercular agents inhibiting mycolylarabinogalactan peptidoglycan (mAGP) assembly.

No. Target Scaffold SAR plan from hit Most advanced analogue In vivo efficacy Ref.
1.1 DprE1 4−Aminoquinolone piperidine amides graphic file with name fcimb-11-611304-g001.jpg graphic file with name fcimb-11-611304-g002.jpg N/Da (Naik et al., 2014)
1.2 Pyrazolopyridones graphic file with name fcimb-11-611304-g003.jpg graphic file with name fcimb-11-611304-g004.jpg N/D (Panda et al., 2014)
1.3 2-Carboxy
quinoxalines
graphic file with name fcimb-11-611304-g005.jpg graphic file with name fcimb-11-611304-g006.jpg N/D (Neres et al., 2015)
1.4 5-Hydroxy pyrimidinediones graphic file with name fcimb-11-611304-g007.jpg graphic file with name fcimb-11-611304-g008.jpg N/D (Oh et al., 2018)
2.1 MmpL3 Adamantyl ureas graphic file with name fcimb-11-611304-g009.jpg graphic file with name fcimb-11-611304-g010.jpg N/D (Brown et al., 2011; North et al., 2013)
2.2 Indolecarboxamides graphic file with name fcimb-11-611304-g011.jpg graphic file with name fcimb-11-611304-g012.jpg Yesb (Onajole et al., 2013; Stec et al., 2016)
2.3 graphic file with name fcimb-11-611304-g013.jpg graphic file with name fcimb-11-611304-g014.jpg Yesb (Kondreddi et al., 2013)
2.4 Tetrahydropyrazolo
pyrimidine carboxamide
graphic file with name fcimb-11-611304-g015.jpg graphic file with name fcimb-11-611304-g016.jpg Yesb (Remuinan et al., 2013; Yokokawa et al., 2013)
2.5 Spirocycles graphic file with name fcimb-11-611304-g017.jpg graphic file with name fcimb-11-611304-g018.jpg Yesb (Remuinan et al., 2013; Guardia et al., 2018)
3.1 MurI Benzoxazoles graphic file with name fcimb-11-611304-g019.jpg graphic file with name fcimb-11-611304-g020.jpg 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.