1.
Bioorg Med Chem Lett
; 17(24): 6797-800, 2007 Dec 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17980587
RESUMEN
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.
Asunto(s)
ARN Polimerasas Dirigidas por ADN/antagonistas & inhibidores , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Lactonas/química , Lactonas/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , ARN Polimerasas Dirigidas por ADN/metabolismo , Inhibidores Enzimáticos/química , Escherichia coli/efectos de los fármacos , Escherichia coli/enzimología , Concentración 50 Inhibidora , Lactonas/síntesis química , Metilación , Estructura Molecular , Staphylococcus aureus/efectos de los fármacos , Staphylococcus aureus/enzimología
2.
Bioorg Med Chem Lett
; 14(22): 5667-72, 2004 Nov 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15482944
RESUMEN
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.