4-Phenyl-1,3-thiazole-2-amines as scaffolds for new antileishmanial agents

Table 2 IC₅₀ values against L. amazonensis promastigotes and the cytotoxicity assay results, expressed as CC₅₀ values

Compound	IC₅₀ (μM)	pIC₅₀	CC₅₀ (μM) THP1 cells^a)	SI	CC₅₀ (μM) L929 cells^b)	SI	CC₅₀ (μM) VERO cells^c)	SI
1	957.56	3.02	143.57	0.15	198.26	0.20	710.06	0.74
2	107.68	3.97	135.40	1.26	159.52	1.48	657.51	6.11
3	46.63	4.33	117.27	2.51	95.45	2.05	1217.5	26.11
4	53.12	4.27	84.65	1.59	121.12	2.28	255.03	4.80
5	53.37	4.27	92.21	1.73	106.08	2.00	511.76	9.59
6	20.78	4.68	45.73	2.20	27.07	1.30	118.17	5.69
7	inactive	inactive	inactive	ND	Inactive	ND	651.29	ND
8	115.95	3.94	82.15	0.70	115.06	0.99	595.94	5.14
Amphotericin B	16.23	–	ND	–	ND	–	ND	–
Pentamidine	10.76	–	ND	–	ND	–	ND	–

(a) THP1 cells: human monocytic cell line derived from acute monocytic leukemia patients; (b) L929 cells: fibroblasts from subcutaneous connective tissue; c) Vero cells: kidney epithelial cells extracted from African green monkeys. IC₅₀: Half-maximal inhibitory concentration on promastigotes; pIC₅₀: Half-maximal inhibitory concentration in log units; CC₅₀: Half cytotoxic concentration; SI: Selectivity Indexes, ND: Not determined. pIC₅₀ calculates as pIC₅₀ = −log₁₀ (IC₅₀)

ISSN: 1678-9199