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Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials.

Gordon S, Simithy J, Goodwin DC, Calderón AI - Perspect Medicin Chem (2015)

Bottom Line: Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK.To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme.In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.

View Article: PubMed Central - PubMed

Affiliation: Department of Drug Discovery and Development, Harrison School of Pharmacy, Auburn University, Auburn, AL, USA.

ABSTRACT
Owing to the persistence of tuberculosis (TB) as well as the emergence of multidrug-resistant and extensively drug-resistant (XDR) forms of the disease, the development of new antitubercular drugs is crucial. Developing inhibitors of shikimate kinase (SK) in the shikimate pathway will provide a selective target for antitubercular agents. Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK. To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme. Currently, there are no data on in vivo activity of Mycobacterium tuberculosis shikimate kinase (MtSK) inhibitors available in the literature. In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.

No MeSH data available.


Related in: MedlinePlus

Pyrazolone analogs.
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Related In: Results  -  Collection


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f6-pmc-7-2015-009: Pyrazolone analogs.

Mentions: The pyrazolone analogs displayed MtSK inhibition at IC50 values lower than 1 μM.31 Based on the structure–activity relationship in the series, the phenyl sulfonamide portion of the molecule is required for the activity, and a single substitution of a halogen at the Para position of the phenyl enhances the MtSK inhibition as for compound 671 (Fig. 6).


Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials.

Gordon S, Simithy J, Goodwin DC, Calderón AI - Perspect Medicin Chem (2015)

Pyrazolone analogs.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4362912&req=5

f6-pmc-7-2015-009: Pyrazolone analogs.
Mentions: The pyrazolone analogs displayed MtSK inhibition at IC50 values lower than 1 μM.31 Based on the structure–activity relationship in the series, the phenyl sulfonamide portion of the molecule is required for the activity, and a single substitution of a halogen at the Para position of the phenyl enhances the MtSK inhibition as for compound 671 (Fig. 6).

Bottom Line: Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK.To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme.In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.

View Article: PubMed Central - PubMed

Affiliation: Department of Drug Discovery and Development, Harrison School of Pharmacy, Auburn University, Auburn, AL, USA.

ABSTRACT
Owing to the persistence of tuberculosis (TB) as well as the emergence of multidrug-resistant and extensively drug-resistant (XDR) forms of the disease, the development of new antitubercular drugs is crucial. Developing inhibitors of shikimate kinase (SK) in the shikimate pathway will provide a selective target for antitubercular agents. Many studies have used in silico technology to identify compounds that are anticipated to interact with and inhibit SK. To a much more limited extent, SK inhibition has been evaluated by in vitro methods with purified enzyme. Currently, there are no data on in vivo activity of Mycobacterium tuberculosis shikimate kinase (MtSK) inhibitors available in the literature. In this review, we present a summary of the progress of SK inhibitor discovery and evaluation with particular attention toward development of new antitubercular agents.

No MeSH data available.


Related in: MedlinePlus