Design, synthesis and structure-activity relationships of 6-O-arylpropargyl diazalides with potent activity against multidrug-resistant Streptococcus pneumoniae

Hong Yong; Yu Gui Gu; Richard F Clark; Thomas Marron; Zhenkun Ma; Niru Soni; Gregory G Stone; Angela M Nilius; Kennan Marsh; Stevan W Djuric

doi:10.1016/j.bmcl.2005.03.011

Design, synthesis and structure-activity relationships of 6-O-arylpropargyl diazalides with potent activity against multidrug-resistant Streptococcus pneumoniae

Bioorg Med Chem Lett. 2005 May 16;15(10):2653-8. doi: 10.1016/j.bmcl.2005.03.011.

Authors

Hong Yong¹, Yu Gui Gu, Richard F Clark, Thomas Marron, Zhenkun Ma, Niru Soni, Gregory G Stone, Angela M Nilius, Kennan Marsh, Stevan W Djuric

Affiliation

¹ Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA. [email protected]

PMID: 15863336
DOI: 10.1016/j.bmcl.2005.03.011

Abstract

A novel series of 6-O-arylpropargyl diazalides was synthesized and evaluated for their antibacterial activity. Members of this series exhibited potent activity against erythromycin-resistant respiratory tract pathogens.

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacokinetics
Anti-Bacterial Agents / pharmacology*
Biological Availability
Drug Resistance, Microbial*
Drug Resistance, Multiple*
Half-Life
Microbial Sensitivity Tests
Propanols / chemical synthesis*
Propanols / chemistry
Propanols / pharmacology*
Streptococcus pneumoniae / drug effects*
Structure-Activity Relationship
Tylosin / analogs & derivatives*
Tylosin / chemical synthesis*
Tylosin / chemistry
Tylosin / pharmacology*

Substances

Anti-Bacterial Agents
Propanols
Tylosin