Department of Applied Chemistry, Kyungpook National University, 80 University Road, Buk-gu, Daegu 702-701, Republic of Korea.
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4315-8. doi: 10.1016/j.bmcl.2013.05.098. Epub 2013 Jun 7.
A series of 3α-amino-5α-cholestane and 3α,7α-diamino-5α-cholestane derivatives containing imidazole and pyridine rings were synthesized by simple and effective reductive amination, and their in vitro activities against a range of Gram-positive and Gram-negative strains were evaluated. Most of the compound exhibited enhanced activity against MRSA pathogen. 3α,7α-Di(pyridylmethyl)amino-5α-cholestane 10 showed the highest potency in these series toward the Gram-positive bacteria, Staphylococcus epidermidis 887E, with the lowest MIC value of 1 μg/mL.
一系列含有咪唑环和吡啶环的 3α-氨基-5α-胆甾烷和 3α,7α-二氨基-5α-胆甾烷衍生物通过简单有效的还原胺化法合成，并评估了它们对一系列革兰氏阳性和革兰氏阴性菌株的体外活性。大多数化合物对 MRSA 病原体的活性增强。在这些系列化合物中，3α,7α-二（吡啶甲基）氨基-5α-胆甾烷 10 对革兰氏阳性菌表皮葡萄球菌 887E 的活性最高，MIC 值最低，为 1μg/mL。
