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Literature summary for 1.13.11.34 extracted from

  • Koeberle, A.; Zettl, H.; Greiner, C.; Wurglics, M.; Schubert-Zsilavecz, M.; Werz, O.
    Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase (2008), J. Med. Chem., 51, 8068-8076.
    View publication on PubMed
Search for more literature for 1.13.11.34

Activating Compound

Activating Compound Comment Organism Structure
additional information Ca2+-ionophore A23187 Homo sapiens

Application

Application Comment Organism
drug development pirinixic acid derivatives constitute a novel class of dual mPGES-1/5-lipoxygenase inhibitors with a promising pharmacologial profile and a potential for therapeutic use Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
Escherichia coli MV1190 transformed with pT3-5LO plasmid Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide BWA4C Homo sapiens
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid
-
 Homo sapiens
2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid
-
 Homo sapiens
2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid
-
 Homo sapiens
2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)acetic acid
-
 Homo sapiens
2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
-
 Homo sapiens
2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
-
 Homo sapiens
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid
-
 Homo sapiens
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid
-
 Homo sapiens
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate
-
 Homo sapiens
additional information class of dual microsomal PGE2 synthase-1/5-lipoxygenase inhibitors based on the structure of pirinixic acid. Target oriented structural modification of pirinixic acid, particularly R substitution with extended n-alkyl or bulky aryl substituents and concomitant replacement of the 2,3-dimethylaniline by a biphenyl-4-yl-methane-amino residue, results in potent suppression of mPGES-1 and 5-lipoxygenase activity. Is not inhibited by 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid Homo sapiens
N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
partially purified by sonication, centrifugation and gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
polymorphonuclear leukocyte
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
arachidonate + O2
-
 Homo sapiens (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyicosa-6,8,11,14-tetraenoate
-
 ?

Synonyms

Synonyms Comment Organism
5-lipoxygenase
-
 Homo sapiens
5-LO
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00011
-
 in intact polymorphonuclear leukocytes Homo sapiens N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide
0.00016
-
 purified 5-lipoxygenase Homo sapiens N-hydroxy-N-[(2E)-3-(3-phenoxyphenyl)prop-2-en-1-yl]acetamide
0.0004
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
0.0005
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
0.0006
-
 in intact polymorphonuclear leukocytes Homo sapiens ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate
0.0007
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid
0.001
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid
0.0015
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid
0.0015
-
 purified 5-lipoxygenase Homo sapiens 2-(4-(biphenyl-4-ylamino)-6-chloropyrimidine-2-ylthio)octanoic acid
0.0015
-
 purified 5-lipoxygenase Homo sapiens 2-(4-chloro-6-(4'-cyanobiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
0.002
-
 purified 5-lipoxygenase Homo sapiens 2-(4-(biphenyl-4-ylmethylamino)-6-chloropyrimidin-2-ylthio)octanoic acid
0.002
-
 purified 5-lipoxygenase Homo sapiens 2-(4-chloro-6-(5-methoxy-2-methylbiphenyl-4-ylamino)pyrimidin-2-ylthio)octanoic acid
0.003
-
 purified 5-lipoxygenase Homo sapiens 2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]octanoic acid
0.0041
-
 in intact polymorphonuclear leukocytes Homo sapiens 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid
0.005
-
 in intact polymorphonuclear leukocytes Homo sapiens ([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(naphthalen-1-yl)acetic acid
0.0065
-
 purified 5-lipoxygenase Homo sapiens 2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)octanoic acid
0.019
-
 purified 5-lipoxygenase Homo sapiens ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]octanoate