LIPOPEPTIDE ANTIFUNGAL AGENTS - AMINE CONJUGATES OF THE SEMISYNTHETICPNEUMOCANDINS L-731,373 AND L-733,560

Authors
ZAMBIAS RA JAMES C ABRUZZO GK BARTIZAL KF HAJDU R THOMPSON R NOLLSTADT KH MARRINAN J BALKOVEC JM
Citation
Ra. Zambias et al., LIPOPEPTIDE ANTIFUNGAL AGENTS - AMINE CONJUGATES OF THE SEMISYNTHETICPNEUMOCANDINS L-731,373 AND L-733,560, Bioorganic & medicinal chemistry letters, 7(15), 1997, pp. 2021-2026
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
15
Year of publication
1997
Pages
2021 - 2026
Database
ISI
SICI code
0960-894X(1997)7:15<2021:LAA-AC>2.0.ZU;2-A
Abstract
Amine conjugates of the semi-synthetic 1,3-beta-(D)-glucan synthesis i nhibitors 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 monoc ationic. The L-ornithine conjugate of 4 possessed excellent pharmacoki netic parameters but lacked sufficient antifungal spectrum for develop ment. (C) 1997 Elsevier Science Ltd.