Table 2.

Combined Biochemical and Antitubercular Evaluation of 1–4.

Compound	R	ClogPb	tPSAb	KD (µM)				Kiapp (µM)	MIC50 (µM)
				MbtA	BasE	EntE	VibE	MbtA	–Fe	+Fe
Fl-Sal-AMSa	n.a.	n.a.	n.a.	0.0093	0.093	0.23	0.13	—	—	—
Sal-AMS		−1.79	210.8	<0.01	<0.1	<0.2	<0.1	0.0066	0.39c	1.56c
1		−0.65	188.5	3.6 ± 0.1	108 ± 8	280 ± 60	98 ± 7	—	>50	>50
2		−0.57	193.4	<0.01	<0.1	0.32 ± 0.04	<0.1	0.12 ± 0.02	>50	>50
3		−1.26	200.9	0.37 ± 0.01	1.19 ± 0.07	12 ± 1	2.5 ± 0.7	—	>50	>50
4		−1.10	208.7	290 ± 70	>300	>300	>300	—	>50	>50

^aStructure of Fl-Sal-AMS:

^bCalculated using ChemBioDraw Ultra Version 13.0.0.3015

^cPreviously reported