Title of article :
Lipopeptide antifungal agents: Amine conjugates of the semi-synthetic pneumocandins L-731,373 and L-733,560
Author/Authors :
Robert A. Zambias، نويسنده , , Catherine James، نويسنده , , George K. Abruzzo، نويسنده , , Kenneth F. Bartizal، نويسنده , , Richard Hajdu، نويسنده , , Randy Thompson، نويسنده , , Karl H. Nollstadt، نويسنده , , Jean Marrinan، نويسنده , , James M. Balkovec، نويسنده ,
Abstract :
Amine conjugates of the semi-synthetic 1,3-β-(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.
