i3S-Instituto de Investigação e Inovação em Saúde, Universidade do Porto, 4200-135 Porto, Portugal.
IBMC-Instituto de Biologia Molecular e Celular, Universidade do Porto, 4200-135 Porto, Portugal.
Int J Mol Sci. 2023 Jan 11;24(2):1402. doi: 10.3390/ijms24021402.
This work reports the synthesis, structural and thermal analysis, and in vitro evaluation of the antimicrobial activity of two new organic salts (OSs) derived from the antimycobacterial drug clofazimine and the fluoroquinolones ofloxacin or norfloxacin. Organic salts derived from active pharmaceutical ingredients (API-OSs), as those herein disclosed, hold promise as cost-effective formulations with improved features over their parent drugs, thus enabling the mitigation of some of their shortcomings. For instance, in the specific case of clofazimine, its poor solubility severely limits its bioavailability. As compared to clofazimine, the clofazimine-derived OSs now reported have improved solubility and thermostability, without any major deleterious effects on the drug's bioactivity profile.
本工作报道了两种新的有机盐(OSs)的合成、结构和热分析,以及体外抗菌活性评价,这两种有机盐源自抗分枝杆菌药物氯法齐明和氟喹诺酮类药物氧氟沙星或诺氟沙星。源自活性药物成分的有机盐(API-OSs),如本文所公开的那样,有望成为具有成本效益的制剂,在改善其母体药物的某些特性的同时,减轻其部分缺点。例如,就氯法齐明而言,其较差的溶解度严重限制了其生物利用度。与氯法齐明相比,现在报道的氯法齐明衍生的 OSs 具有改善的溶解度和热稳定性,而对药物的生物活性谱没有任何重大的有害影响。