Tuberculosis is one of the ten causes of morbidity and mortality worldwide caused by Mycobacterium tuberculosis complex. Some of the anti-tuberculosis drugs used in clinic studies, despite being effective for the treatment of tuberculosis, present serious adverse effects as well as poor bioavailability, stability, and drug-resistance problems. Thus, it is important to develop approaches that could provide shorter drug regimens, preventing drug resistance, toxicity of the antibiotics, and improve their bioavailability. Herein, we reported the use of organic salts based on the isoniazid drug, which can act as an organic cation combined with suitable organic anions such as alkylsulfonate-based (mesylate, R or S-Camphorsulfonate), carboxylate-based (glycolate, vanylate) and sacharinate. The synthesis, characterization, and cytotoxicity studies comparing with the original isoniazid drug have been performed. The possibility to explore dicationic salts seems promising in order to improve original bioavailability, and promote the elimination of polymorphic forms as well as higher stability, which are relevant characteristics that the pharmaceutical industry pursues.

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基于异烟肼药物的有机盐：合成，生物利用度和细胞毒性研究

结核是全世界由结核分枝杆菌引起的发病率和死亡率的十大原因之一复杂。临床研究中使用的一些抗结核药物尽管对治疗结核病有效，但仍存在严重的不良反应以及不良的生物利用度，稳定性和耐药性问题。因此，重要的是开发出可以提供更短的药物治疗方案，预防耐药性，抗生素毒性并提高其生物利用度的方法。在本文中，我们报道了基于异烟肼药物的有机盐的使用，该药物可以作为有机阳离子与合适的有机阴离子结合使用，例如烷基磺酸盐基（甲磺酸盐，R或S-樟脑磺酸盐），羧酸盐基（乙醇酸盐，钒酸盐）和糖精。与原始异烟肼药物相比，已经进行了合成，表征和细胞毒性研究。