Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine

Jamie L. Cohen; Agenor Limon; Ricardo Miledi; A. Richard Chamberlin

doi:10.1016/j.bmcl.2006.01.047

Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine

Jamie L. Cohen, Agenor Limon, Ricardo Miledi, A. Richard Chamberlin

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

24 Scopus citations

Abstract

The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (-)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.

Original language	English (US)
Pages (from-to)	2189-2194
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2006.01.047
State	Published - Apr 15 2006
Externally published	Yes

Keywords

Dysiherbaine
Excitatory amino acid receptors
KA receptor agonist
KA reeptor antagonist
NMDA receptor agonist
Scaffold

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2006.01.047

Cite this

@article{ed57069b606a4ed9a34f62d2fb4346ef,

title = "Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine",

abstract = "The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (-)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.",

keywords = "Dysiherbaine, Excitatory amino acid receptors, KA receptor agonist, KA reeptor antagonist, NMDA receptor agonist, Scaffold",

author = "Cohen, {Jamie L.} and Agenor Limon and Ricardo Miledi and Chamberlin, {A. Richard}",

year = "2006",

month = apr,

day = "15",

doi = "10.1016/j.bmcl.2006.01.047",

language = "English (US)",

volume = "16",

pages = "2189--2194",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "8",

}

TY - JOUR

T1 - Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine

AU - Cohen, Jamie L.

AU - Limon, Agenor

AU - Miledi, Ricardo

AU - Chamberlin, A. Richard

PY - 2006/4/15

Y1 - 2006/4/15

N2 - The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (-)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.

AB - The design and synthesis of four 2,2-disubstituted dihydrobenzofurans that are structurally related to several glutamate-containing natural products, including (-)-dysiherbaine, is described. Biological evaluation of these analogs shows that one is a KA receptor antagonist and another is an NMDA receptor agonist.

KW - Dysiherbaine

KW - Excitatory amino acid receptors

KW - KA receptor agonist

KW - KA reeptor antagonist

KW - NMDA receptor agonist

KW - Scaffold

UR - http://www.scopus.com/inward/record.url?scp=33644804186&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=33644804186&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.01.047

DO - 10.1016/j.bmcl.2006.01.047

M3 - Article

C2 - 16455241

AN - SCOPUS:33644804186

SN - 0960-894X

VL - 16

SP - 2189

EP - 2194

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine

Abstract

Keywords

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this