使穆伦多菌素鸟氨酸单元上的半缩醛胺功能稳定的方法。

Approaches towards the stabilization of hemiaminal function at ornithine unit of mulundocandin.

作者信息

Lal Bansi, Gund Vitthal Genbhau

机构信息

Quest Institute of LifeScience, Nicholas Piramal India Limited, and Hoechst Research Center, Mulund, Mumbai-400080, Maharashtra, India.

出版信息

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1123-8. doi: 10.1016/j.bmcl.2003.12.084.

DOI:10.1016/j.bmcl.2003.12.084

PMID:14980649

Abstract

Semisynthetic modifications at position-12 (ornithine-5-position, hemiaminal function) of mulundocandin were carried out to improve its chemical stability. New carbon-carbon (C-C) and carbon-hydrogen (C-H) linkage at hemiaminal function -12 has been achieved. Lewis acid catalyzed introduction of electron rich aryl group at position-12 of mulundocandin is developed. Synthesized mulundocandin analogues were evaluated for their chemical stability and antifungal activity against C. albicans and A. fumigatus.

摘要

对穆伦多坎菌素12位（鸟氨酸-5位，半缩醛胺官能团）进行半合成修饰以提高其化学稳定性。已在半缩醛胺官能团-12处实现了新的碳-碳（C-C）和碳-氢（C-H）键连接。开发了路易斯酸催化在穆伦多坎菌素12位引入富电子芳基的方法。对合成的穆伦多坎菌素类似物进行了化学稳定性以及针对白色念珠菌和烟曲霉的抗真菌活性评估。