Scholars@Duke publication: Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine

Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine

Publication , Journal Article

Bergnest, G; Kaddurah-Daouk, R

Published in: Bioorganic and Medicinal Chemistry Letters

April 22, 1997

The first hydrolytically stable phosphocreatine (CrP) analogs with a CH2-P isostere in place of the NH-P linkage have been synthesized and found to inhibit creatine kinase (CK) with potencies in the low mM range. The closest structural analog of CrP, 2, was found to have a K(i) (1.4 mM) near the K(m) of CrP (2.5 mM), making it the most potent known reversible inhibitor of CK.

Duke Scholars

Author Rima Fathi Kaddurah-Daouk Psychiatry & Behavioral Sciences, Behavioral Medicine & Neur ...

Published In

Bioorganic and Medicinal Chemistry Letters

DOI

10.1016/S0960-894X(97)00161-3

ISSN

0960-894X

Publication Date

April 22, 1997

Volume

Issue

Start / End Page

1021 / 1026

Related Subject Headings

Medicinal & Biomolecular Chemistry
3405 Organic chemistry
3404 Medicinal and biomolecular chemistry
1115 Pharmacology and Pharmaceutical Sciences
0305 Organic Chemistry
0304 Medicinal and Biomolecular Chemistry

Citation

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Bergnest, G., & Kaddurah-Daouk, R. (1997). Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters, 7(8), 1021–1026. https://doi.org/10.1016/S0960-894X(97)00161-3

Bergnest, G., and R. Kaddurah-Daouk. “Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine.” Bioorganic and Medicinal Chemistry Letters 7, no. 8 (April 22, 1997): 1021–26. https://doi.org/10.1016/S0960-894X(97)00161-3.

Bergnest G, Kaddurah-Daouk R. Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters. 1997 Apr 22;7(8):1021–6.

Bergnest, G., and R. Kaddurah-Daouk. “Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine.” Bioorganic and Medicinal Chemistry Letters, vol. 7, no. 8, Apr. 1997, pp. 1021–26. Scopus, doi:10.1016/S0960-894X(97)00161-3.

Bergnest G, Kaddurah-Daouk R. Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters. 1997 Apr 22;7(8):1021–1026.

Published In

Bioorganic and Medicinal Chemistry Letters

DOI

10.1016/S0960-894X(97)00161-3

ISSN

0960-894X

Publication Date

April 22, 1997

Volume

Issue

Start / End Page

1021 / 1026

Related Subject Headings

Medicinal & Biomolecular Chemistry
3405 Organic chemistry
3404 Medicinal and biomolecular chemistry
1115 Pharmacology and Pharmaceutical Sciences
0305 Organic Chemistry
0304 Medicinal and Biomolecular Chemistry