Jamison J A, Zeckner D J, Rodriguez M J
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA.
J Antibiot (Tokyo). 1997 Jul;50(7):562-6. doi: 10.7164/antibiotics.50.562.
The synthesis and biological activity of a series of N-alkylated derivatives of echinocandin B are described and compared with the N-acylated analogs. The linear, rigid geometry of the side chain that was essential to improve the antifungal potency of the N-acylated series gave similar in vitro results with the N-alkylated derivatives. However the slight structural variation forfeited all in vivo activity.
描述了一系列棘白菌素B的N-烷基化衍生物的合成及其生物活性，并与N-酰化类似物进行了比较。对于提高N-酰化系列抗真菌效力至关重要的侧链线性刚性几何结构，在N-烷基化衍生物中产生了相似的体外结果。然而，轻微的结构变化使所有体内活性丧失。
