Synthesis and antibacterial activity of O-substituted nocathiacin I derivatives

B Narasimhulu Naidu; Margaret E Sorenson; Thomas Hudyma; Xiaofan Zheng; Yunhui Zhang; Joanne J Bronson; Michael J Pucci; Junius M Clark; Yasutsugu Ueda

doi:10.1016/j.bmcl.2004.04.102

Synthesis and antibacterial activity of O-substituted nocathiacin I derivatives

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3743-6. doi: 10.1016/j.bmcl.2004.04.102.

Authors

B Narasimhulu Naidu¹, Margaret E Sorenson, Thomas Hudyma, Xiaofan Zheng, Yunhui Zhang, Joanne J Bronson, Michael J Pucci, Junius M Clark, Yasutsugu Ueda

Affiliation

¹ The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]

PMID: 15203154
DOI: 10.1016/j.bmcl.2004.04.102

Abstract

The synthesis and antibacterial activity of a series of new nocathiacin I derivatives (1-12) containing polar water solubilizing groups is described. Most of these compounds exhibited potent antibacterial activity and have improved water solubility. In addition, compounds 5, 7-9 also exhibited potent in vivo activity.

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / pharmacology
Enterococcus faecalis / drug effects
Intercellular Signaling Peptides and Proteins
Microbial Sensitivity Tests
Peptides / chemical synthesis*
Peptides / pharmacology
Solubility
Staphylococcus aureus / drug effects
Streptococcus pneumoniae / drug effects
Structure-Activity Relationship
Water / chemistry

Substances

Anti-Bacterial Agents
Intercellular Signaling Peptides and Proteins
Peptides
nocathiacin I
Water