| dc.contributor.author |
Magrioti, V |
en |
| dc.contributor.author |
Nikolaou, A |
en |
| dc.contributor.author |
Smyrniotou, A |
en |
| dc.contributor.author |
Shah, I |
en |
| dc.contributor.author |
Constantinou-Kokotou, V |
en |
| dc.contributor.author |
Dennis, EA |
en |
| dc.contributor.author |
Kokotos, G |
en |
| dc.date.accessioned |
2014-06-06T06:52:42Z |
|
| dc.date.available |
2014-06-06T06:52:42Z |
|
| dc.date.issued |
2013 |
en |
| dc.identifier.issn |
09680896 |
en |
| dc.identifier.uri |
http://dx.doi.org/10.1016/j.bmc.2013.07.010 |
en |
| dc.identifier.uri |
http://62.217.125.90/xmlui/handle/123456789/6137 |
|
| dc.subject |
GVIA iPLA2 |
en |
| dc.subject |
Inhibitor |
en |
| dc.subject |
Pentafluoroethyl ketones |
en |
| dc.subject |
Phospholipase A2 |
en |
| dc.subject |
Polyfluoroalkyl ketone |
en |
| dc.subject.other |
1,1 difluoro 5 phenylpentan 2 one |
en |
| dc.subject.other |
1,1 difluoro 6 phenylhexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 (2 methoxyphenyl)hexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 (4 fluorophenyl)hexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 (4 methoxyphenyl)hexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 (6 methoxynaphthalen 1 yl)hexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 (naphthalen 1 yl)hexan 2 one |
en |
| dc.subject.other |
1,1,1 trifluoro 6 [4 (trifluoromethyl)phenyl]hexan 2 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoro 7 (2 methoxyphenyl)heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoro 7 (4 flurophenyl)heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoro 7 (4 methoxyphenyl)heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoro 7 (naphthalen 1 yl)heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoro 7 [4 (trifluoromethyl)phenyl]heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2 pentafluoroheptan 7 (6 methoxynaphthalen 2 yl)heptan 3 one |
en |
| dc.subject.other |
1,1,1,2,2,3,3 heptafluoro 8 (naphthalen 1 yl)octan 4 one |
en |
| dc.subject.other |
4 (biphenyl 2 yl) 1,1,1 trifluorobutan 2 one |
en |
| dc.subject.other |
5 (biphenyl 2 yl) 1,1,1,2,2 pentafluoropentan 3 one |
en |
| dc.subject.other |
6 (2,4 dimethoxyphenyl) 1,1,1 trifluorohexan 2 one |
en |
| dc.subject.other |
6 (3,4 dimethoxyphenyl) 1,1,1 trifluorohexan 2 one |
en |
| dc.subject.other |
6 (benzo[d][1,3]dioxo 5 yl) 1,1,1 trifluorohexan 2 one |
en |
| dc.subject.other |
6 (biphenyl 4 yl) 1,1,1 trifluorohexan 2 one |
en |
| dc.subject.other |
7 (2,4 dimethoxyphenyl) 1,1,1,2,2 pentafluoroheptan 3 one |
en |
| dc.subject.other |
7 (3,4 dimethoxyphenyl) 1,1,1,2,2 pentafluoroheptan 3 one |
en |
| dc.subject.other |
7 (benzo[d][1,3]dioxol 5 yl) 1,1,1,2,2 pentafluoroheptan 3 one |
en |
| dc.subject.other |
7 (biphenyl 4 yl) 1,1,1,2,2 pentafluoroheptan 3 one |
en |
| dc.subject.other |
calcium independent phospholipase A2 |
en |
| dc.subject.other |
calcium independent phospholipase A2 inhibitor |
en |
| dc.subject.other |
esterase inhibitor |
en |
| dc.subject.other |
unclassified drug |
en |
| dc.subject.other |
article |
en |
| dc.subject.other |
drug potency |
en |
| dc.subject.other |
enzyme inhibition |
en |
| dc.subject.other |
in vitro study |
en |
| dc.subject.other |
structure activity relation |
en |
| dc.subject.other |
structure analysis |
en |
| dc.subject.other |
GVIA iPLA(2) |
en |
| dc.subject.other |
Inhibitor |
en |
| dc.subject.other |
Pentafluoroethyl ketones |
en |
| dc.subject.other |
Phospholipase A(2) |
en |
| dc.subject.other |
Polyfluoroalkyl ketone |
en |
| dc.subject.other |
Fluorine |
en |
| dc.subject.other |
Group VI Phospholipases A2 |
en |
| dc.subject.other |
Ketones |
en |
| dc.subject.other |
Phospholipase A2 Inhibitors |
en |
| dc.subject.other |
Protein Binding |
en |
| dc.subject.other |
Protein Isoforms |
en |
| dc.title |
New potent and selective polyfluoroalkyl ketone inhibitors of GVIA calcium-independent phospholipase A2 |
en |
| heal.type |
journalArticle |
en |
| heal.identifier.primary |
10.1016/j.bmc.2013.07.010 |
en |
| heal.publicationDate |
2013 |
en |
| heal.abstract |
Group VIA calcium-independent phospholipase A2 (GVIA iPLA 2) has recently emerged as an important pharmaceutical target. Selective and potent GVIA iPLA2 inhibitors can be used to study its role in various neurological disorders. In the current work, we explore the significance of the introduction of a substituent in previously reported potent GVIA iPLA2 inhibitors. 1,1,1,2,2-Pentafluoro-7-(4-methoxyphenyl) heptan-3-one (GK187) is the most potent and selective GVIA iPLA2 inhibitor ever reported with a XI(50) value of 0.0001, and with no significant inhibition against GIVA cPLA2 or GV sPLA2. We also compare the inhibition of two difluoromethyl ketones on GVIA iPLA 2, GIVA cPLA2, and GV sPLA2. © 2013 Elsevier Ltd. All rights reserved. |
en |
| heal.journalName |
Bioorganic and Medicinal Chemistry |
en |
| dc.identifier.issue |
18 |
en |
| dc.identifier.volume |
21 |
en |
| dc.identifier.doi |
10.1016/j.bmc.2013.07.010 |
en |
| dc.identifier.spage |
5823 |
en |
| dc.identifier.epage |
5829 |
en |