SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL 3'-HTY-SUBSTITUTED PNEUMOCANDINS

Authors
BLACK RM BALKOVEC JM NOLLSTADT KM DREIKORN S BARTIZAL KF ABRUZZO GK
Citation
Rm. Black et al., SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NOVEL 3'-HTY-SUBSTITUTED PNEUMOCANDINS, Bioorganic & medicinal chemistry letters, 7(22), 1997, pp. 2879-2884
Citations number
17
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
22
Year of publication
1997
Pages
2879 - 2884
Database
ISI
SICI code
0960-894X(1997)7:22<2879:SASON3>2.0.ZU;2-C
Abstract
A series of pneumocandin B-0 analogs substituted at the 3'-position of the homotyrosine (Hty) residue have been prepared and evaluated for t heir inhibition of 1,3-beta-(D)-glucan synthesis and for their antifun gal activity against C. albicans. Cationic analogs displayed enhanced antifungal properties. The phenolic hydroxyl is involved in a critical hydrogen-bond at the binding site of the enzyme. (C) 1997 Elsevier Sc ience Ltd.