Solid-phase synthesis and anti-infective activity of a combinatorial library based on the natural product anisomycin.
The solid-phase synthesis of a library based on the natural product anisomycin is described. The resulting library was tested against a panel of bacterial and fungal targets, and active compounds were identified in a Staphylococcus aureus whole-cell assay and an efflux-deficient fungal whole-cell assay.
Shi
Shuhao
S
New Leads Chemistry, 5 Research Parkway, Wallingford, CT 06492, USA. shij@bms.com
Zhu
Shirong
S
Gerritz
Samuel W
SW
Esposito
Kim
K
Padmanabha
Ramesh
R
Li
Wenying
W
Herbst
John J
JJ
Wong
Henry
H
Shu
Yue Zhong
YZ
Lam
Kin S
KS
Sofia
Michael J
MJ
D000841:Anisomycin / Q000737:chemistry*; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001688:Biological Products / Q000737:chemistry*; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D005658:Fungi / Q000166:cytology / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000166:cytology / Q000187:drug effects; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D001688:Biological Products; D000841:Anisomycin