N-取代的1,4-恶唑并庚因基索德菌素作为选择性真菌EF-2抑制剂的合成与评价
Synthesis and evaluation of N-substituted 1,4-oxazepanyl Sordaricins as selective fungal EF-2 inhibitors.
作者信息
Kaneko Satoru, Arai Masami, Uchida Takuya, Harasaki Tamako, Fukuoka Takashi, Konosu Toshiyuki
机构信息
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., 2-58, Hiromachi 1-chome, Shinagawa-ku, Tokyo 140-8710, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Jul 8;12(13):1705-8. doi: 10.1016/s0960-894x(02)00290-1.
Sordaricin analogues possessing 6-methoxy-7-methyl-1,4-oxazepane moiety instead of the sugar part were synthesized and evaluated. It was found that N-substituents on the oxazepane ring had influence on biological activity. In particular, N-(2-methylpropenyl) derivative 12p exhibited potent in vitro antifungal activity. Furthermore, 12p maintained significant activity (MIC 0.25 microg/mL) against Candida albicans SANK51486 even in the presence of 20% horse serum.
合成并评估了具有6-甲氧基-7-甲基-1,4-恶唑烷部分而非糖部分的索达里辛类似物。发现恶唑烷环上的N-取代基对生物活性有影响。特别是，N-(2-甲基丙烯基)衍生物12p表现出强大的体外抗真菌活性。此外，即使在存在20%马血清的情况下，12p对白色念珠菌SANK51486仍保持显著活性（MIC为0.25微克/毫升）。
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