Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin; Alexandre Mongeot; Russell Collighan; Robert E. Saint; Richard A. Jones; Ian G.C. Coutts; Daniel L. Rathbone

doi:10.1016/j.bmcl.2008.09.006

Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin, Alexandre Mongeot, Russell Collighan, Robert E. Saint, Richard A. Jones, Ian G.C. Coutts, Daniel L. Rathbone

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

Abstract

Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

Original language	English
Pages (from-to)	5559-5562
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.09.006
Publication status	Published - 15 Oct 2008

Keywords

transglutaminase
inhibitors
dipeptide

Access to Document

10.1016/j.bmcl.2008.09.006

Cite this

@article{9dbd3cec8c874a50b6f067dcfbd91186,

title = "Synthesis of potent water-soluble tissue transglutaminase inhibitors",

abstract = "Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.",

keywords = "transglutaminase, inhibitors, dipeptide",

author = "Martin Griffin and Alexandre Mongeot and Russell Collighan and Saint, {Robert E.} and Jones, {Richard A.} and Coutts, {Ian G.C.} and Rathbone, {Daniel L.}",

year = "2008",

month = oct,

day = "15",

doi = "10.1016/j.bmcl.2008.09.006",

language = "English",

volume = "18",

pages = "5559--5562",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier",

number = "20",

}

TY - JOUR

T1 - Synthesis of potent water-soluble tissue transglutaminase inhibitors

AU - Griffin, Martin

AU - Mongeot, Alexandre

AU - Collighan, Russell

AU - Saint, Robert E.

AU - Jones, Richard A.

AU - Coutts, Ian G.C.

AU - Rathbone, Daniel L.

PY - 2008/10/15

Y1 - 2008/10/15

N2 - Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

AB - Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.

KW - transglutaminase

KW - inhibitors

KW - dipeptide

UR - http://www.scopus.com/inward/record.url?scp=53349166956&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2008.09.006

DO - 10.1016/j.bmcl.2008.09.006

M3 - Article

SN - 0960-894X

VL - 18

SP - 5559

EP - 5562

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Synthesis of potent water-soluble tissue transglutaminase inhibitors

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this