Design, synthesis and biological evaluation of simplified side chains of the macrolide antibiotic etnangien

Mario Altendorfer; Herbert Irschik; Dirk Menche

doi:10.1016/j.bmcl.2012.06.070

Design, synthesis and biological evaluation of simplified side chains of the macrolide antibiotic etnangien

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5731-4. doi: 10.1016/j.bmcl.2012.06.070. Epub 2012 Jul 14.

Authors

Mario Altendorfer¹, Herbert Irschik, Dirk Menche

Affiliation

¹ Organische Chemie, Ruprecht-Karls-Universität Heidelberg, INF 270, D-69120 Heidelberg, Germany.

PMID: 22832317
DOI: 10.1016/j.bmcl.2012.06.070

Abstract

Novel simplified side chains of the potent RNA polymerase inhibitor etnangien were designed, synthesized and evaluated for antibacterial activity against Gram-positive bacteria and one Gram-negative bacterium.

Publication types

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

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacology*
DNA-Directed RNA Polymerases / antagonists & inhibitors*
Drug Design
Gram-Negative Bacteria / drug effects
Gram-Negative Bacteria / enzymology
Gram-Negative Bacterial Infections / drug therapy
Gram-Positive Bacteria / drug effects*
Gram-Positive Bacteria / enzymology
Gram-Positive Bacterial Infections / drug therapy
Macrolides / chemical synthesis
Macrolides / chemistry*
Macrolides / pharmacology*
Polyenes / chemical synthesis
Polyenes / chemistry*
Polyenes / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Macrolides
Polyenes
etnangien
DNA-Directed RNA Polymerases