Table 1. Enzyme affinity and parasitic LE for mono- and bicyclic analogues 1, 5 and 6 .

No.	Structure	clog P a	PfNMT		PvNMT		LdNMT		HsNMT K i (μM)
			K i (μM)	LE b	K i (μM)	LE	K i (μM)	LE
1		4.0	0.83	0.30	0.08	0.35	5.82	0.28	3.20
5		2.9	>100	—	6.50	0.30	0.73	0.35	>100
6		3.0	6.00	0.29	2.42	0.31	0.28	0.36	>100

^aclog P values calculated with ChemAxon.

^bLE = [–log(K _i)](1.374)/(no. of heavy atoms).