Riccardin C derivatives as anti-MRSA agents: structure-activity relationship of a series of hydroxylated bis(bibenzyl)s

Hiromi Sawada; Miki Okazaki; Daichi Morita; Teruo Kuroda; Kenji Matsuno; Yuichi Hashimoto; Hiroyuki Miyachi

doi:10.1016/j.bmcl.2012.10.052

Riccardin C derivatives as anti-MRSA agents: structure-activity relationship of a series of hydroxylated bis(bibenzyl)s

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7444-7. doi: 10.1016/j.bmcl.2012.10.052. Epub 2012 Oct 17.

Authors

Hiromi Sawada¹, Miki Okazaki, Daichi Morita, Teruo Kuroda, Kenji Matsuno, Yuichi Hashimoto, Hiroyuki Miyachi

Affiliation

¹ Division of Pharmaceutical Sciences, Okayama University, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, 1-1-1, Tsushima-Naka, Kita-ku, Okayama 700-8530, Japan.

PMID: 23122868
DOI: 10.1016/j.bmcl.2012.10.052

Abstract

Members of a series of macrocyclic bis(bibenzyl) riccardin-class derivatives were found to exhibit antibacterial activity towards methicillin-resistant Staphylococcus aureus (anti-MRSA activity). Structure-activity relationship (SAR) studies were conducted, focusing on the number and position of the hydroxyl groups. The minimum essential structure for anti-MRSA activity was also investigated.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Dose-Response Relationship, Drug
Ethers, Cyclic / chemical synthesis
Ethers, Cyclic / chemistry
Ethers, Cyclic / pharmacology*
Methicillin-Resistant Staphylococcus aureus / drug effects*
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Ethers, Cyclic
riccardin C