ChemMedChem. 2010 Feb 1;5(2):286-95.

5-Benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligases.

Tomasić T, Zidar N, Kovac A, Turk S, Simcic M, Blanot D, Müller-Premru M, Filipic M, Grdadolnik SG, Zega A, Anderluh M, Gobec S, Kikelj D, Peterlin Masic L.

Source

University of Ljubljana, Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia.

Abstract

Mur ligases participate in the intracellular path of bacterial peptidoglycan biosynthesis and constitute attractive, although so far underexploited, targets for antibacterial drug discovery. A series of hydroxy-substituted 5-benzylidenethiazolidin-4-ones were synthesized and tested as inhibitors of Mur ligases. The most potent compound 5 a was active against MurD-F with IC(50) values between 2 and 6 microm, making it a promising multitarget inhibitor of Mur ligases. Antibacterial activity against different strains, inhibitory activity against protein kinases, mutagenicity and genotoxicity of 5 a were also investigated, and kinetic and NMR studies were conducted.

PMID:: 20024979; [PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Medical

Antibiotics - MedlinePlus Health Information

Supplemental Content

Related citations

Synthesis and biological evaluation of N-acylhydrazones as inhibitors of MurC and MurD ligases. [ChemMedChem. 2008]
Synthesis and biological evaluation of N-acylhydrazones as inhibitors of MurC and MurD ligases.
Sink R, Kovac A, Tomasić T, Rupnik V, Boniface A, Bostock J, Chopra I, Blanot D, Masic LP, Gobec S, et al. ChemMedChem. 2008 Sep; 3(9):1362-70.
Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase. [Bioorg Med Chem Lett. 2009]
Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligase.
Tomasić T, Zidar N, Rupnik V, Kovac A, Blanot D, Gobec S, Kikelj D, Masic LP. Bioorg Med Chem Lett. 2009 Jan 1; 19(1):153-7. Epub 2008 Nov 5.
Discovery of new inhibitors of the bacterial peptidoglycan biosynthesis enzymes MurD and MurF by structure-based virtual screening. [Bioorg Med Chem. 2009]
Discovery of new inhibitors of the bacterial peptidoglycan biosynthesis enzymes MurD and MurF by structure-based virtual screening.
Turk S, Kovac A, Boniface A, Bostock JM, Chopra I, Blanot D, Gobec S. Bioorg Med Chem. 2009 Mar 1; 17(5):1884-9. Epub 2009 Jan 29.
Review Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents. [Curr Med Chem. 2005]
Review Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents.
Jain R, Chen D, White RJ, Patel DV, Yuan Z. Curr Med Chem. 2005; 12(14):1607-21.
Review Structure and function of the Mur enzymes: development of novel inhibitors. [Mol Microbiol. 2003]
Review Structure and function of the Mur enzymes: development of novel inhibitors.
El Zoeiby A, Sanschagrin F, Levesque RC. Mol Microbiol. 2003 Jan; 47(1):1-12.

See reviews... See all...

Related information

Related Citations
Calculated set of PubMed citations closely related to the selected article(s) retrieved using a word weight algorithm. Related articles are displayed in ranked order from most to least relevant, with the “linked from” citation displayed first.
Substance (MeSH Keyword)
PubChem chemical substance (submitted) records that are classified under the same Medical Subject Headings (MeSH) controlled vocabulary as the current articles.

Recent activity

Clear Turn Off Turn On

5-Benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligas...
5-Benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligases.
ChemMedChem. 2010 Feb 1 ;5(2):286-95.

PubMed
Scheduled maintenance treatment with infliximab is superior to episodic treatmen...
Scheduled maintenance treatment with infliximab is superior to episodic treatment for the healing of mucosal ulceration associated with Crohn's disease.
Gastrointest Endosc. 2006 Mar ;63(3):433-42; quiz 464.

PubMed
The effect of vitamin K2 on bone metabolism in aged female rats.
The effect of vitamin K2 on bone metabolism in aged female rats.
Osteoporos Int. 2005 Dec ;16(12):1604-10. Epub 2005 Apr 22 .

PubMed
Evaluation of the aldosterone-blocking agent eplerenone in hypertension and hear...
Evaluation of the aldosterone-blocking agent eplerenone in hypertension and heart failure.
Expert Opin Pharmacother. 2007 Dec ;8(17):3053-9.

PubMed
Adiponectin replenishment ameliorates obesity-related hypertension.
Adiponectin replenishment ameliorates obesity-related hypertension.
Hypertension. 2006 Jun ;47(6):1108-16. Epub 2006 May 1 .

PubMed

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

PubMed

Display Settings:

Send to:

5-Benzylidenethiazolidin-4-ones as multitarget inhibitors of bacterial Mur ligases.

Source

Abstract

Publication Types, MeSH Terms, Substances

Publication Types

MeSH Terms

Substances

LinkOut - more resources

Full Text Sources

Medical

Supplemental Content

Related citations

Related information

Recent activity

Simple NCBI Directory

Getting Started

Resources

Popular

Featured

NCBI Information