Design and Synthesis of Novel Antileishmanial Compounds

Table 2

Cyclized substances and heterocyclic structures as terminal substituents with a side chain length of 4 carbon atoms; given bioactivities are against promastigotes of L. major in comparison to the reference substances miltefosine (1) and pentamidine (2).

Compound		R^1	R^2	R^3	R^4	Bioactivity
17						Inactive
18						Inactive
11	1	Me		Boc	Bn	Active
12	1	Me		H	Bn	Active
29	1	Me		Boc	Bn	Inactive
30	1	Me		Boc	Bn	Inactive
14	1	H		Boc	Bn	Active
15	1	H		Boc	H	Inactive
27	1	Me		Boc	H	Inactive
28	1	Me		Boc	Bn	Inactive
40	1	H		Boc	Bn	Active