Table 4. SAR of analogues with 2-methoxyphenyl LHS.

R	Compound	Ld InMac pEC50 a	THP-1 pEC50 a	Aqueous solubility b μM	Cli mouse, c ml min–1 g–1
	20	7.1	4.4	<1	5.0
	37	6.7	<4.3	<1	14
	38	6.3	4.4	24	14
	39	6.4	<4.3	ND d	9
	40	5.7	<4.3	79	2
	41	6.8	<4.3	412	3.4
	42	6.5	4.4	22	1.6
	43	7.6	4.8	53	6.3

^aLd InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigotes.9 Data are the mean values for n ≥ 3 replicates and standard deviations are ≤0.4.

^bAq. solubility is kinetic aqueous solubility (CAD).11

^cCl_i is mouse liver microsomal intrinsic clearance.10

^dND means not determined.