Synthesis and screening of small molecule inhibitors of anthrax edema factor

Maria Estrella Jimenez; Kathryn Bush; Jennifer Pawlik; Laurie Sower; Johnny W. Peterson; Scott R. Gilbertson

doi:10.1016/j.bmcl.2008.05.059

Synthesis and screening of small molecule inhibitors of anthrax edema factor

Maria Estrella Jimenez, Kathryn Bush, Jennifer Pawlik, Laurie Sower, Johnny W. Peterson, Scott R. Gilbertson

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts of the prostaglandin PGE₂ reduce the net secretory response of cholera toxin-challenged mice and act directly on the action of anthrax edema factor, a calmodulin-dependent adenylyl cyclase. The simple enones examined in this letter were prepared by palladium-catalyzed Suzuki reaction.

Original language	English (US)
Pages (from-to)	4215-4218
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2008.05.059
State	Published - Jul 15 2008
Externally published	Yes

Keywords

Adeylyl cyclase
Antrhax
Edema factor

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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10.1016/j.bmcl.2008.05.059

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title = "Synthesis and screening of small molecule inhibitors of anthrax edema factor",

abstract = "The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts of the prostaglandin PGE2 reduce the net secretory response of cholera toxin-challenged mice and act directly on the action of anthrax edema factor, a calmodulin-dependent adenylyl cyclase. The simple enones examined in this letter were prepared by palladium-catalyzed Suzuki reaction.",

keywords = "Adeylyl cyclase, Antrhax, Edema factor",

author = "Jimenez, {Maria Estrella} and Kathryn Bush and Jennifer Pawlik and Laurie Sower and Peterson, {Johnny W.} and Gilbertson, {Scott R.}",

note = "Funding Information: This work was supported by the Mission Pharmacal and the Robert A. Welch Foundation and Mission Pharmcal. ",

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T1 - Synthesis and screening of small molecule inhibitors of anthrax edema factor

AU - Jimenez, Maria Estrella

AU - Bush, Kathryn

AU - Pawlik, Jennifer

AU - Sower, Laurie

AU - Peterson, Johnny W.

AU - Gilbertson, Scott R.

N1 - Funding Information: This work was supported by the Mission Pharmacal and the Robert A. Welch Foundation and Mission Pharmcal.

PY - 2008/7/15

Y1 - 2008/7/15

N2 - The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts of the prostaglandin PGE2 reduce the net secretory response of cholera toxin-challenged mice and act directly on the action of anthrax edema factor, a calmodulin-dependent adenylyl cyclase. The simple enones examined in this letter were prepared by palladium-catalyzed Suzuki reaction.

AB - The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts of the prostaglandin PGE2 reduce the net secretory response of cholera toxin-challenged mice and act directly on the action of anthrax edema factor, a calmodulin-dependent adenylyl cyclase. The simple enones examined in this letter were prepared by palladium-catalyzed Suzuki reaction.

KW - Adeylyl cyclase

KW - Antrhax

KW - Edema factor

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AN - SCOPUS:47149086946

SN - 0960-894X

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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ER -

Synthesis and screening of small molecule inhibitors of anthrax edema factor

Abstract

Keywords

ASJC Scopus subject areas

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