Design, Antileishmanial Activity, and QSAR Studies of a Series of Piplartine Analogues

Table 1

Antileishmanial activity of compounds 5–36 against the strains IFLA/BR/1967/PH8 of Leishmania (L.) amazonensis.

Cinnamic esters			Amides			Benzoic esters
	IC50; (μM)	SI		IC50; (μM)	SI		IC50; (μM)	SI
5	0.641 ± 0.052	>0.154	22	0.577 ± 0.080	>0.148	35	>0.656 ± 0.05	>0.141
6	0.257 ± 0.041	>0.364	23	0.091 ± 0.015	>0.126	36	>0.02 ± 0.0	>3.205
7	0.09 ± 0.032	>0.992	24	0.564 ± 0.061	>0.126
8	0.194 ± 0.04	>0.459	25	0.117 ± 0.027	>0.678
9	0.149 ± 0.025	>0.570	26	0.734 ± 0.252	>0.104
10	0.133 ± 0.014	>0.608	27	0.353 ± 0.080	>0.243
11	0.076 ± 0.009	>0.868	28	0.109 ± 0.010	>0.063
12	0.076 ± 0.022	>1.106	29	0.662 ± 0.188	>0.105
13	0.101 ± 0.031	>0.688	30	1.137 ± 0.252	>0.062
14	0.975 ± 0.241	>0.069	31	>1.108	>0.062
15	0.125 ± 0.035	>0.561	32	0.486 ± 0.043	>0.127
16	0.513 ± 0.065	>0.142	33	>1.033	>0.062
17	0.083 ± 0.016	>0.748	34	>1.033	>0.062
18	0.029 ± 0.007	>2.688
19	>1.041	>0.062
20	0.007 ± 0.008	>10			Positive control: amphotericin B		0.0015
21	0.042 ± 0.011	>1.582	-

Cytotoxic effects on MRC5 (Medical Research Council cell strain 5—fibroblast derived from lung tissue); positive control: doxorubicin (IC₅₀ 0.00287 (0.0017–0.0050) μM). SI: selectivity index.