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  • Title: Anti-tubercular agents. Part 3. Benzothiadiazine as a novel scaffold for anti-Mycobacterium activity.
    Author: Kamal A, Reddy KS, Ahmed SK, Khan MN, Sinha RK, Yadav JS, Arora SK.
    Journal: Bioorg Med Chem; 2006 Feb 01; 14(3):650-8. PubMed ID: 16203154.
    Abstract:
    In an effort to develop new and more effective therapies to treat tuberculosis, a series of benzothiadiazine 1,1-dioxide derivatives were synthesized and their in vitro activity against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium intracellulare was evaluated. One of the compounds, 8c, exhibited potent anti-tubercular activity, particularly for the resistant strains and thus prompted us to investigate its in vivo profile. However, the in vivo testing in a mouse model of tuberculosis infection did not show significant anti-tubercular activity, probably because of its poor bioavailability.
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