Lipopeptide antifungal agents: Amine conjugates of the semi-synthetic pneumocandins L-731,373 and L-733,560

被引：5

作者：

Zambias, RA

James, C

Abruzzo, GK

Bartizal, KF

Hajdu, R

Thompson, R

Nollstadt, KH

Marrinan, J

Balkovec, JM

机构：

[1] MERCK RES LABS,DEPT MED CHEM,RAHWAY,NJ 07065

[2] MERCK RES LABS,DEPT INFECT DIS RES,RAHWAY,NJ 07065

[3] MERCK RES LABS,DEPT PARASITE BIOCHEM & CELL BIOL,RAHWAY,NJ 07065

[4] MERCK RES LABS,DEPT ANTIBIOT DISCOVERY & DEV,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(97)00359-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amine conjugates of the semi-synthetic 1,3-beta-(D)-glucan synthesis inhibitors L-731,373 (3) and L-733,560 (4) were prepared and evaluated for in vitro and in vivo antifungal activity. Tricationic analogs were more potent than the dicationic which were more potent than the monocationic. The L-ornithine conjugate of 4 possessed excellent pharmacokinetic parameters but lacked sufficient antifungal spectrum for development. (C) 1997 Elsevier Science Ltd.

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页码：2021 / 2026

页数：6

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