1.
Bioorg Med Chem Lett
; 17(24): 6797-800, 2007 Dec 15.
Article
in English
| MEDLINE
| ID: mdl-17980587
ABSTRACT
Based upon observations from our initial findings, additional myxopyronin B analogs have been prepared and tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against Escherichia coli and Staphylococcus aureus.
Subject(s)
DNA-Directed RNA Polymerases/antagonists & inhibitors , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Lactones/chemistry , Lactones/pharmacology , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , DNA-Directed RNA Polymerases/metabolism , Enzyme Inhibitors/chemistry , Escherichia coli/drug effects , Escherichia coli/enzymology , Inhibitory Concentration 50 , Lactones/chemical synthesis , Methylation , Molecular Structure , Staphylococcus aureus/drug effects , Staphylococcus aureus/enzymology
2.
Bioorg Med Chem Lett
; 14(22): 5667-72, 2004 Nov 15.
Article
in English
| MEDLINE
| ID: mdl-15482944
ABSTRACT
A series of myxopyronin B analogs has been prepared via a convergent synthetic route and were tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against E. coli and S. aureus. The parent lead compound proved to be very sensitive to even small changes. Only the achiral desmethyl myxopyronin B (1a) provided enhanced potency.
