Design and Synthesis of Novel Antileishmanial Compounds

Table 1

Plain open-chain aliphatic structures with diverse terminal substituents and altered side chain lengths; 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
6						Inactive
5	1	Me	Br	Boc	Bn	Active
7	1	=CH2	H	Boc	Bn	Inactive
8	1	Me	N3	Boc	Bn	Active
9	1	Me	N3	H	Bn	Inactive
10	1	Me	NH2	Boc	Bn	Inactive
19	1	H	Br	Boc	Bn	Inactive
20	7	H	Br	Boc	Bn	Active
21	0	=CH2	H	Boc	Bn	Active
22	6	=CH2	H	Boc	Bn	Inactive
23	1	H	N3	Boc	Bn	Inactive
24	7	H	N3	Boc	Bn	Inactive
25	1	H	NH2	Boc	Bn	Inactive
26	7	H	NH2	Boc	Bn	Active