1. Anti-infection
  2. Parasite
  3. Antitrypanosomal agent 32

Antitrypanosomal agent 32 is a antitrypanosomal agent with nanomolar potency against multiple Trypanosoma cruzi strains, including CL-Brener, Y, Dm28c-Luc and Tulahuen. Antitrypanosomal agent 32 sustains inhibition of parasite growth after washing and reduces parasitemia levels in BALB/c mice. Antitrypanosomal agent 32 can be used for the research of trypanosome infection.

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Antitrypanosomal agent 32

Antitrypanosomal agent 32 Chemical Structure

CAS No. : 1916476-01-1

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Description

Antitrypanosomal agent 32 is a antitrypanosomal agent with nanomolar potency against multiple Trypanosoma cruzi strains, including CL-Brener, Y, Dm28c-Luc and Tulahuen. Antitrypanosomal agent 32 sustains inhibition of parasite growth after washing and reduces parasitemia levels in BALB/c mice. Antitrypanosomal agent 32 can be used for the research of trypanosome infection[1].

IC50 & Target[1]

Trypanosoma

 

In Vitro

Antitrypanosomal agent 32 (compound 2) inhibits Trypanosoma cruzi Tulahuen strain intracellular amastigotes in L929 cells with an IC50 of 5.4 μM and has a selectivity index of 46 relative to L929 cell cytotoxicity[1].
Antitrypanosomal agent 32 inhibits Trypanosoma cruzi Dm28c-Luc strain intracellular amastigotes in Vero cells with an IC50 of 4.9 μM and IC90 of 36 μM, with selectivity indexes >61 and >8 respectively due to no detected cytotoxicity in Vero cells[1].
Antitrypanosomal agent 32 inhibits Trypanosoma cruzi Y strain intracellular amastigotes in L6 cells with an IC50 of 0.16 μM and has a selectivity index of >1875 relative to L6 cell cytotoxicity[1].
Antitrypanosomal agent 32 inhibits Trypanosoma cruzi CL-Brener-Luc strain intracellular amastigotes in L6 cells with an IC50 of 0.036 μM and IC90 of 0.094 μM, with selectivity indexes >8333 and >3191 respectively due to no detected cytotoxicity in L6 cells[1].
Antitrypanosomal agent 32 (36-125 μM; 3 days post-washout) exhibits trypanocidal activity against Trypanosoma cruzi Dm28c-Luc strain in Vero cells, with 92.6% and 95.2% growth inhibition 3 days after washout from IC90 (36 μM) and 125 μM exposures respectively[1].
Antitrypanosomal agent 32 (0.094-1 μM; 10 days post-washout) exhibits trypanocidal activity against Trypanosoma cruzi CL-Brener-Luc strain in L6 cells, with 89.4% and 99.6% growth inhibition 10 days after washout from IC90 (0.094 μM) and 1 μM exposures respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Antitrypanosomal agent 32 (compound 2) (10-50 mg/kg; i.p.; daily; 10 days) achieves an 84% maximum reduction in parasitemia in female BALB/c mice with acute Chagas disease, with no observed acute toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (female, acute Chagas disease model infected with Trypanosoma cruzi CL-Brener-Luc trypomastigotes)[1]
Dosage: 10 mg/kg (first 5 days); 50 mg/kg (subsequent 5 days)
Administration: i.p.; daily; 10 days
Result: Reduced parasitemia persistently from day 7 post-infection throughout treatment.
Lowered parasitemia by about 50% at day 13 and maximally by 84% at day 17 post-infection.
Preserved steady body weight with no acute toxicity or mortality.
Molecular Weight

317.41

Formula

C16H19N3O2S

CAS No.
SMILES

O=C(N1CCOCC1)NCCC2=NC(C3=CC=CC=C3)=CS2

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