Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential enzyme for parasite survival. In view of triclosan’s poor druggability, which limits its therapeutic use, a new set of B-ring modified analogs were designed to optimize its physico-chemical properties. These derivatives were synthesized and evaluated by in vitro assay and TgENR enzyme assay. Some analogs display improved solubility, permeability and a comparable MIC50 value to that of triclosan. Modeling of these inhibitors revealed the same overall binding mode with the enzyme as triclosan, but the B-ring modifications have additional interactions with the strongly conserved Asn130
Toxoplasma gondii is an obligate intracellular parasite with global incidence. The acute infection, ...
University of Minnesota M.S. thesis. April 2013. Major: Chemistry. Advisor: Peter Grundt. 1 computer...
Drug treatment for toxoplasmosis is problematic, because current drugs cannot eradicate latent infec...
Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential ...
Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by...
Many microbial pathogens rely on a type II fatty acid synthesis (FASII) pathway that is distinct fro...
Through our focused effort to discover new and effective agents against toxoplasmosis, a structure-b...
The enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of apicomple...
The protozoan parasite Toxoplasma gondii is the causative agent of one of the most widespread parasi...
Recent studies have demonstrated that submicromolar concentrations of the biocide triclosan arrest t...
Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by...
AbstractThe enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of a...
Enoyl acyl carrier protein reductase enzyme (ENR) catalyses one of the two reductive steps in fatty ...
This article reports anti-Toxoplasma gondii activity of 3-(thiophen-2-yl)-1,2,4-triazole-5-thione. T...
AbstractThe enoyl acyl-carrier protein reductase (ENR) enzyme of the apicomplexan parasite family ha...
Toxoplasma gondii is an obligate intracellular parasite with global incidence. The acute infection, ...
University of Minnesota M.S. thesis. April 2013. Major: Chemistry. Advisor: Peter Grundt. 1 computer...
Drug treatment for toxoplasmosis is problematic, because current drugs cannot eradicate latent infec...
Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential ...
Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by...
Many microbial pathogens rely on a type II fatty acid synthesis (FASII) pathway that is distinct fro...
Through our focused effort to discover new and effective agents against toxoplasmosis, a structure-b...
The enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of apicomple...
The protozoan parasite Toxoplasma gondii is the causative agent of one of the most widespread parasi...
Recent studies have demonstrated that submicromolar concentrations of the biocide triclosan arrest t...
Toxoplasmosis causes significant morbidity and mortality, and yet available medicines are limited by...
AbstractThe enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of a...
Enoyl acyl carrier protein reductase enzyme (ENR) catalyses one of the two reductive steps in fatty ...
This article reports anti-Toxoplasma gondii activity of 3-(thiophen-2-yl)-1,2,4-triazole-5-thione. T...
AbstractThe enoyl acyl-carrier protein reductase (ENR) enzyme of the apicomplexan parasite family ha...
Toxoplasma gondii is an obligate intracellular parasite with global incidence. The acute infection, ...
University of Minnesota M.S. thesis. April 2013. Major: Chemistry. Advisor: Peter Grundt. 1 computer...
Drug treatment for toxoplasmosis is problematic, because current drugs cannot eradicate latent infec...