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首页> 外文期刊>Archiv der Pharmazie >Rifalazil and other benzoxazinorifamycins in the treatment of Chlamydia-based persistent infections.
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Rifalazil and other benzoxazinorifamycins in the treatment of Chlamydia-based persistent infections.

机译：利福拉齐和其他苯并恶嗪利福霉素治疗衣原体持续感染。

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摘要

Rifalazil is a benzoxazinorifamycin which inhibits bacterial DNA-dependent RNA polymerase. The benzoxazine ring endows benzoxazinorifamycins with unique physical and chemical characteristics which favor the use of rifalazil and derivatives in treating diseases caused by the obligate intracellular pathogens of the genus chlamydia. Minimal inhibitory concentrations of benzoxazinorifamycins against chlamydia are in the pg/mL range. These compounds have potential as monotherapeutic agents to treat chlamydia-associated disease because they retain activity against chlamydia strains resistant to currently approved rifamycins such as rifampin. A pivotal clinical trial with rifalazil has been initiated for the treatment of peripheral arterial disease. The rationale for this innovative use of rifalazil, including the association of C. pneumoniae in atherosclerotic plaque formation, as well as rifalazil's potency and efficacy against chlamydia in both preclinical and clinical studies, is discussed. Other benzoxazino derivatives may have utility as stand-alone topical antibacterials or combination antibacterials to treat serious Gram-positive infections. None of the benzoxaminorifamycins examined to date induce the cytochrome P450 3A4 enzyme. This is in contrast to currently approved rifamycins which are strong inducers of P450 enzymes, resulting in drug-drug interactions that limit the clinical utility of this drug class.
机译：利福拉齐是一种抑制细菌DNA依赖性RNA聚合酶的苯并恶嗪利福霉素。苯并恶嗪环赋予苯并恶嗪利福霉素独特的物理和化学特性，有利于利福拉齐及其衍生物用于治疗由衣原体属的专性细胞内病原体引起的疾病。苯并恶嗪利福霉素对衣原体的最小抑制浓度在pg / mL范围内。这些化合物作为治疗衣原体相关疾病的单一治疗剂具有潜力，因为它们保留了对目前批准的利福霉素（如利福平）耐药的衣原体菌株的活性。利福拉齐的一项关键性临床试验已经启动，用于治疗周围动脉疾病。讨论了利福拉齐这种创新用途的基本原理，包括肺炎衣原体与动脉粥样硬化斑块形成的关系，以及利福拉齐在临床前和临床研究中对抗衣原体的效力和功效。其他苯并恶嗪衍生物可作为独立的局部抗菌药或联合抗菌药用于治疗严重的革兰氏阳性感染。迄今为止，没有检查过的苯并氨基氨基利福霉素诱导细胞色素P450 3A4酶。这与目前批准的利福霉素相反，后者是P450酶的强诱导剂，导致药物与药物的相互作用限制了该药物类别的临床应用。

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