Table 2. Activity values/properties of NMT inhibitors from DDD85646 series.^* .

	IC50 L. donovani NMT	EC50 extracellular L. donovani amastigotes	EC50 intracellular L. donovani amastigotes	LD50 bone marrow derived macrophages	pKa	cLogP	Hydrogen bond donors
DDD85646 1	3.6 nM	8 µM	n.p.	>45 µM	8.8	2.0	2
DDD100887 2	20 nM	660 nM	190 nM	23 µM	8.8	4.2	1
DDD86211 2	7.3 nM	180 nM	n.p.	>45 µM	6.5	2.4	1

¹resynthesised DDD85646 (Ref 31).

²resynthesised from WO2010/026365 [Ref 37].

*structures shown in Fig. 4A.

n.p. – not possible.