Abstract
3-Substituted-5-(4-pyridylcarboxamide)tetrahydro-2H-[1,3,5]thiadizine-2-thione derivatives (1-9) were synthesized as derivatives of isoniazid (INH) to overcome the resistance developed with its therapeutic use. The structures were confirmed by their spectral and elemental analyses data. These derivatives revealed higher lipophilicity compared with INH. The antimycobacterial activity of the synthesized compounds and INH was evaluated in vitro against Mycobacterium tuberculosis H37Rv at 6.25 µg/ml in BACTEC 12B medium using the BACTEC 460 radiometric system. The derivatives exhibited antitubercular activity.
Highlights
Tuberculosis is considered by the WHO, to be the most important chronic communicabledisease in the world [I]
Rapid glance to the obtained results revealed that the prodrugs 1-9 exhibited antimycobacterial activity
The lipophilicity of the synthesized p r o d ~ g sincreased remarkably compared with the parent drug, INH
Summary
Tuberculosis is considered by the WHO, to be the most important chronic communicabledisease in the world [I]. In spite of toxicity on repeated dosing isoniazid (INH) is still considered to be a first line drug for chemotherapy of tuberculosis [6]. It was suggested that the mechanism of resistance to INH is related to a failure of the drug to penetrate or to be taken up by the microorganisms [7]. Resistance development to a drug can be obviated through prodrug approach [9, 101. Tetrahydro-2H-[l,3,5]thiadiazine-2-thione derivatives were found to insinuate the criterion of the prodrug approach that impart the desirable physicochemical properties to attached drugs, and liberate the parent drugs through chemical or enzymatic degradation [ I 1-13]. The current work describes the incorporation of INH in a tetrahydro-2H[I,3, 5lthiadiazine-2-thione moiety (THTT)
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