Benzimidazole and aminoalcohol derivatives show in vitro anthelmintic activity against Trichuris muris and Heligmosomoides polygyrus

Table 3 Base structure and results of L₁ assays for benzimidazole (BZ) derivatives against T. muris

	Compound		T. muris L₁ assay		Cytotoxicity		Selectivity Indexes
Compound identification	R¹	R²	% dead larvae (100 µM)	IC₅₀ (µM)	Caco 2 CC₅₀ (µM)	HepG2 CC₅₀ (µM)	SI Caco2	SI HepG2
BZ1	Me	4´-OMe	100.00	15.92	11.60 ± 3.42	18.75 ± 1.92	< 1	1.18
BZ2	Me	4´-Cl	91.29	21.94	28.06 ± 1.35	27.11 ± 1.69	1.28	1.23
BZ3	Me	2´,6´-diMe	73.90	–	9.14 ± 2.32	> 25	–	–
BZ4	Me	3´-NO₂,4´-OMe	40.67	–	9.07 ± 2.35	> 25	–	–
BZ5	Cl	4´-OMe	71.85	–	37.38 ± 3.38	36.03 ± 3.02	–	–
BZ6	Cl	4´-Cl	90.80	4.17	22.58 ± 1.69	17.54 ± 0.91	5.41	4.21
BZ7	Cl	4´- NO₂	54.74	–	19.14 ± 2.05	21.73 ± 1.65	–	–
BZ8	Cl	2´,6´-diMe	46.82	–	23.28 ± 2.47	30.22 ± 3.35	–	–
BZ9	Cl	3´-NO₂,4´-OMe	52.43	–	67.31 ± 15.31	53.43 ± 16.61	–	–
BZ10	Cl	3´-NH₂,4´-OMe	62.06	–	34.70 ± 4.32	44.91 ± 5.94	–	–
BZ11	NO₂	4´-OMe	53.37		14.37 ± 3.69	22.98 ± 19.57	–	–
BZ12	NO₂	4´-Cl	95.00	8.89	12.29 ± 1.09	14.64 ± 0.83	1.38	1.65
BZ13	NO₂	2´,6´-diMe	99.40	18.53	16.78 ± 9.16	> 12.5	< 1	< 1
BZ14	NO₂	3´-NO₂,4´-OMe	55.24	–	13.38 ± 3.02	13.64 ± 4.85	–	–
BZ15	NH₂	4´–OMe	42.26	–	> 25	> 50	–	–

Cytotoxicity data were reported in previous study [19]
CC₅₀: cytotoxic concentration 50; IC₅₀: inhibitory concentration 50; Me: methyl; R: radical; SI: selectivity index. SI = CC₅₀ (Caco-2 or HepG2)/IC₅₀

ISSN: 1756-3305