Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics

B Narasimhulu Naidu; Margaret E Sorenson; Yunhui Zhang; Oak K Kim; John D Matiskella; John A Wichtowski; Timothy P Connolly; Wenying Li; Kin S Lam; Joanne J Bronson; Michael J Pucci; Junius M Clark; Yasutsugu Ueda

doi:10.1016/j.bmcl.2004.08.058

Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5573-7. doi: 10.1016/j.bmcl.2004.08.058.

Authors

B Narasimhulu Naidu¹, Margaret E Sorenson, Yunhui Zhang, Oak K Kim, John D Matiskella, John A Wichtowski, Timothy P Connolly, Wenying Li, Kin S Lam, 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: 15482927
DOI: 10.1016/j.bmcl.2004.08.058

Abstract

Several nocathiacin I analogues (4-35) were synthesized and evaluated for their antibacterial activity. Most of these semi-synthetic analogues retained very good in vitro and in vivo antibacterial activity of 1.

MeSH terms

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

Substances

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