Solid-phase synthesis and anti-infective activity of a combinatorial library based on the natural product anisomycin

Shuhao Shi; Shirong Zhu; Samuel W Gerritz; Kim Esposito; Ramesh Padmanabha; Wenying Li; John J Herbst; Henry Wong; Yue Zhong Shu; Kin S Lam; Michael J Sofia

doi:10.1016/j.bmcl.2005.06.004

Solid-phase synthesis and anti-infective activity of a combinatorial library based on the natural product anisomycin

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4151-4. doi: 10.1016/j.bmcl.2005.06.004.

Authors

Shuhao Shi¹, Shirong Zhu, Samuel W Gerritz, Kim Esposito, Ramesh Padmanabha, Wenying Li, John J Herbst, Henry Wong, Yue Zhong Shu, Kin S Lam, Michael J Sofia

Affiliation

¹ New Leads Chemistry, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]

PMID: 16005213
DOI: 10.1016/j.bmcl.2005.06.004

Abstract

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.

MeSH terms

Anisomycin / chemistry*
Anti-Infective Agents / chemical synthesis*
Anti-Infective Agents / chemistry
Anti-Infective Agents / pharmacology*
Biological Products / chemistry*
Cell Line
Combinatorial Chemistry Techniques*
Fungi / cytology
Fungi / drug effects
Humans
Inhibitory Concentration 50
Molecular Structure
Staphylococcus aureus / cytology
Staphylococcus aureus / drug effects
Structure-Activity Relationship

Substances

Anti-Infective Agents
Biological Products
Anisomycin