Cargando…
Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents
A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthesis of bacterial cell-walls. Some compounds po...
Autores principales: | , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2008
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245483/ https://www.ncbi.nlm.nih.gov/pubmed/18259126 http://dx.doi.org/10.3390/molecules13010011 |
_version_ | 1783372250943062016 |
---|---|
author | Frlan, Rok Kovač, Andreja Blanot, Didier Gobec, Stanislav Pečar, Slavko Obreza, Aleš |
author_facet | Frlan, Rok Kovač, Andreja Blanot, Didier Gobec, Stanislav Pečar, Slavko Obreza, Aleš |
author_sort | Frlan, Rok |
collection | PubMed |
description | A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthesis of bacterial cell-walls. Some compounds possessed inhibitory activity against both enzymes with IC(50) values as low as 30 μM. In addition, a new, one-pot synthesis of amidobenzaldehydes is reported. |
format | Online Article Text |
id | pubmed-6245483 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2008 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62454832018-11-26 Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents Frlan, Rok Kovač, Andreja Blanot, Didier Gobec, Stanislav Pečar, Slavko Obreza, Aleš Molecules Full Paper A series of novel N-benzylidenesulfonohydrazide compounds were designed and synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) and UDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved in the biosynthesis of bacterial cell-walls. Some compounds possessed inhibitory activity against both enzymes with IC(50) values as low as 30 μM. In addition, a new, one-pot synthesis of amidobenzaldehydes is reported. MDPI 2008-01-11 /pmc/articles/PMC6245483/ /pubmed/18259126 http://dx.doi.org/10.3390/molecules13010011 Text en © 2008 by MDPI (http://www.mdpi.org). Reproduction is permitted for noncommercial purposes. |
spellingShingle | Full Paper Frlan, Rok Kovač, Andreja Blanot, Didier Gobec, Stanislav Pečar, Slavko Obreza, Aleš Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title | Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title_full | Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title_fullStr | Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title_full_unstemmed | Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title_short | Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents |
title_sort | design and synthesis of novel n-benzylidenesulfonohydrazide inhibitors of murc and murd as potential antibacterial agents |
topic | Full Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245483/ https://www.ncbi.nlm.nih.gov/pubmed/18259126 http://dx.doi.org/10.3390/molecules13010011 |
work_keys_str_mv | AT frlanrok designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents AT kovacandreja designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents AT blanotdidier designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents AT gobecstanislav designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents AT pecarslavko designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents AT obrezaales designandsynthesisofnovelnbenzylidenesulfonohydrazideinhibitorsofmurcandmurdaspotentialantibacterialagents |