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  4. Ditophal

Ditophal is an orally active thiol ester anti-tuberculosis and anti-leprosy agent. Ditophal combats Mycobacterium tuberculosis infections in subcutaneous and intracerebral sites in guinea pigs, including isoniazid (HY-B0329)-resistant strains. Ditophal alters the staining characteristics of Mycobacterium leprae and reduces the bacterial index of leprosy. Ditophal causes ulcers at the injection site when administered subcutaneously to guinea pigs at high doses. Ditophal can be used in the research of tuberculosis and leprosy.

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Ditophal

Ditophal Chemical Structure

CAS No. : 584-69-0

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Description

Ditophal is an orally active thiol ester anti-tuberculosis and anti-leprosy agent. Ditophal combats Mycobacterium tuberculosis infections in subcutaneous and intracerebral sites in guinea pigs, including isoniazid (HY-B0329)-resistant strains. Ditophal alters the staining characteristics of Mycobacterium leprae and reduces the bacterial index of leprosy. Ditophal causes ulcers at the injection site when administered subcutaneously to guinea pigs at high doses. Ditophal can be used in the research of tuberculosis and leprosy[1][2].

In Vivo

Ditophal (100-200 mg/kg; p.o.; twice daily; for 90 consecutive days) reduces the organ severity score of tuberculosis and prolongs the survival time of guinea pigs subcutaneously infected with Mycobacterium tuberculosis[1].
Ditophal (10-50 mg/kg; subcutaneous injection; daily or weekly; for 120 consecutive days) reduces the tuberculosis organ severity score and prolongs the survival time of guinea pigs subcutaneously infected with Mycobacterium tuberculosis[1].
Ditophal (100-200 mg/kg; p.o.; twice daily; for 4 consecutive weeks) prolongs the average survival time of guinea pigs with intracerebral Mycobacterium tuberculosis infection, and the 100 mg/kg dose group shows a longer average survival time of up to 35.0 days[1].

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

Animal Model: Guinea-pigs (434 to 648 g weight; subcutaneous Mycobacterium tuberculosis infection)[1]
Dosage: 200 mg/kg; 100 mg/kg
Administration: p.o.; two doses daily; until 90th day after infection (no treatment on Saturdays or Sundays)
Result: Produced mean total tuberculosis organ score of 7.7 (lung 1.3, liver 0, spleen 2.0, bronchial lymph nodes 4.3) and mean survival time of 99.7 days when started on infection day at 200 mg/kg.
Produced mean total tuberculosis organ score of 9.0 (lung 2.3, liver 1.3, spleen 1.3, bronchial lymph nodes 4.0) and mean survival time of 120 days when started 14 days post-infection at 200 mg/kg.
Produced mean total tuberculosis organ score of 11.3 (lung 2.3, liver 1.3, spleen 2.7, bronchial lymph nodes 5.0) and mean survival time of 81.3 days when started on infection day at 100 mg/kg.
Produced mean total tuberculosis organ score of 9.0 (lung 1.0, liver 0.5, spleen 2.5, bronchial lymph nodes 5.0) and mean survival time of 97.0 days when started 14 days post-infection at 100 mg/kg.
Animal Model: Guinea-pigs (440 to 630 g weight; subcutaneous Mycobacterium tuberculosis infection)[1]
Dosage: 50 mg/kg; 10 mg/kg
Administration: s.c.; once daily or once weekly; until 120th day after infection
Result: Produced mean total tuberculosis organ score of 14.0 (lung 1.7, liver 3.4, spleen 4.3, bronchial lymph nodes 4.6) and mean survival time of 118 days at 50 mg/kg once daily.
Produced mean total tuberculosis organ score of 16.2 (lung 3.9, liver 4.25, spleen 3.8, bronchial lymph nodes 4.4) and mean survival time of 88.6 days at 50 mg/kg once weekly.
Produced mean total tuberculosis organ score of 15.25 (lung 3.9, liver 3.75, spleen 3.5, bronchial lymph nodes 4.1) and mean survival time of 100 days at 10 mg/kg once daily.
Produced mean total tuberculosis organ score of 13.6 (lung 4.1, liver 2.5, spleen 2.75, bronchial lymph nodes 4.25) and mean survival time of 100 days at 10 mg/kg once weekly.
Animal Model: Guinea-pigs (238 to 472 g weight; intracerebral Mycobacterium tuberculosis infection)[1]
Dosage: 200 mg/kg; 100 mg/kg
Administration: p.o.; two doses daily; 4 weeks (started day after infection)
Result: Produced mean survival time of 28.5 days at 200 mg/kg.
Produced mean survival time of 35.0 days at 100 mg/kg.
Molecular Weight

254.36

Formula

C12H14O2S2
CAS No.
SMILES

O=C(SCC)C1=CC=CC(=C1)C(=O)SCC
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Keywords:

Ditophal584-69-0EtisulBacterialMycobacterium tuberculosisisoniazid-resistant strainsleprosytuberculosisMycobacterium lepraeDDSleprosy bacterial indexguinea-pigsInhibitorinhibitorinhibit

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