Brufani M, Cellai L, Cozzella L, Federici M, Guiso M, Segre A
J Antibiot (Tokyo). 1985 Oct;38(10):1359-62. doi: 10.7164/antibiotics.38.1359.
Rifamycins inhibit bacterial DNA-dependent RNA polymerase through the formation of non-covalent bonds by the oxygenated groups at C(1), C(8), C(21), and C(23). These must be unhindered and underivatized, with the antibiotic in a proper overall molecular conformation. The present study shows that contrary to previous conclusions the availability of the hydroxyl group at C(21) is not as important as that of the other three groups. In support of this is the observation that 21-epi-rifamycin S is partially active, both on the isolated DNA-dependent RNA polymerase and on some Gram-positive bacterial strains.
利福霉素通过其C(1)、C(8)、C(21)和C(23)位的含氧基团形成非共价键来抑制细菌的DNA依赖性RNA聚合酶。这些基团必须是无阻碍的且未衍生化的，同时抗生素需处于合适的整体分子构象。本研究表明，与先前的结论相反，C(21)位羟基的可及性不如其他三个基团重要。支持这一观点的观察结果是，21-表-利福霉素S对分离的DNA依赖性RNA聚合酶和一些革兰氏阳性细菌菌株都有部分活性。
