135 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase.
University Jena
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.
Peking University
Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase.
University of Naples
Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase.
Friedrich-Schiller-University
Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.
Harvard Medical School
One-step semisynthesis of oleacein and the determination as a 5-lipoxygenase inhibitor.
University of Athens
Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.
National Institutes of Health
Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.
Guru Nanak Dev University
Discovery and biological evaluation of novel 1,4-benzoquinone and related resorcinol derivatives that inhibit 5-lipoxygenase.
University of Salerno
Inhibition of LOX by flavonoids: a structure-activity relationship study.
Universidade Do Porto
Novel di-tertiary-butyl phenylhydrazones as dual cyclooxygenase-2/5-lipoxygenase inhibitors: synthesis, COX/LOX inhibition, molecular modeling, and insights into their cytotoxicities.
Medical University of South Carolina
Exploring the chemical space of multitarget ligands using aligned self-organizing maps.
Goethe University
Discovery of a novel activator of 5-lipoxygenase from an anacardic acid derived compound collection.
University of Groningen
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
Goethe-University Frankfurt
Investigating the selectivity of metalloenzyme inhibitors.
University of California San Diego
Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.
Pfizer
Synthesis and structure-activity relationship studies of novel dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase.
Goethe-University Frankfurt
N-1, C-3 substituted indoles as 5-LOX inhibitors--in vitro enzyme immunoaasay, mass spectral and molecular docking investigations.
Guru Nanak Dev University
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
Ici Pharmaceuticals Group
Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases.
Groningen Research Institute of Pharmacy
Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.
Eberhard-Karls University
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
Zafes/Liff/Goethe University Frankfurt
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.
Peking University
Charting, navigating, and populating natural product chemical space for drug discovery.
Max Planck Institute of Molecular Physiology
Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.
University of Innsbruck
Synthesis of benzo-annulated tryptanthrins and their biological properties.
Yeungnam University
Design and synthesis of a second series of triazole-based compounds as potent dual mPGES-1 and 5-lipoxygenase inhibitors.
University of Salerno
Dual-target virtual screening by pharmacophore elucidation and molecular shape filtering.
TBA
Synthesis and biological evaluation of a class of 5-benzylidene-2-phenyl-thiazolinones as potent 5-lipoxygenase inhibitors.
Zafes/Liff/Osf Goethe-University Frankfurt
A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors.
Goethe-University Frankfurt
Using enzyme assays to evaluate the structure and bioactivity of sponge-derived meroterpenes.
University of California Santa Cruz
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.
Eberhard Karls University Tuebingen
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.
Merck Frosst Centre For Therapeutic Research
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
The Scripps Research Institute
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.
Abbott Laboratories
Substituted (pyridylmethoxy)naphthalenes as potent and orally active 5-lipoxygenase inhibitors; synthesis, biological profile, and pharmacokinetics of L-739,010.
Merck Frosst Centre For Therapeutic Research
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
Abbott Laboratories
Dioxabicyclooctanyl naphthalenenitriles as nonredox 5-lipoxygenase inhibitors: structure-activity relationship study directed toward the improvement of metabolic stability.
Merck Frosst Centre For Therapeutic Research
(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor.
Abbott Laboratories
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.
R. W. Johnson Pharmaceutical Research Institute
Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.
Ici Pharmaceuticals Group
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
Wyeth-Ayerst Research
A study of novel antiallergic agents with eosinophilic infiltration inhibiting action.
Tokushima Bunri University
SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase.
Zafes/Liff/Osf Goethe-University Frankfurt
Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
University of Hyderabad
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Amira Pharmaceuticals
Bioassay-guided identification of an anti-inflammatory prenylated acylphloroglucinol from Melicope ptelefolia and molecular insights into its interaction with 5-lipoxygenase.
Universiti Putra Malaysia
Design, synthesis and biological evaluation of benzo[1.3.2]dithiazolium ylide 1,1-dioxide derivatives as potential dual cyclooxygenase-2/5-lipoxygenase inhibitors.
National Taiwan University
Pyrazol-3-propanoic acid derivatives as novel inhibitors of leukotriene biosynthesis in human neutrophils.
Gazi University
Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.
National Human Genome Research Institute
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.
Bristol-Myers Squibb Research and Development
Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1.
Eberhard Karls University Tuebingen
Pharmacophore modeling and virtual screening for novel acidic inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1).
University of Innsbruck
Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro.
University of Veterinary and Pharmaceutical Sciences Brno
Structure-based discovery of inhibitors of microsomal prostaglandin E2 synthase-1, 5-lipoxygenase and 5-lipoxygenase-activating protein: promising hits for the development of new anti-inflammatory agents.
University of Salerno
A novel class of dual mPGES-1/5-LO inhibitors based on thea-naphthyl pirinixic acid scaffold.
Goethe-University Frankfurt
Identifying chelators for metalloprotein inhibitors using a fragment-based approach.
University of California
Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286.
Merck Frosst Centre For Therapeutic Research
Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.
National Human Genome Research Institute
Design, synthesis, and biological evaluation of prenylated chalcones as 5-LOX inhibitors.
University of Hyderabad
Bioactivity-guided mapping and navigation of chemical space.
Institut FüR Molekulare Physiologie
Derivatives of schisandrin with increased inhibitory potential on prostaglandin E(2) and leukotriene B(4) formation in vitro.
University of Graz
Discovery of 3-(4-bromophenyl)-6-nitrobenzo[1.3.2]dithiazolium ylide 1,1-dioxide as a novel dual cyclooxygenase/5-lipoxygenase inhibitor that also inhibits tumor necrosis factor-alpha production.
National Taiwan University
Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4-formation.
Karl-Franzens-Universit£T Graz
O-alkylcarboxylate oxime and N-hydroxyurea analogs of substituted indole leukotriene biosynthesis inhibitors
TBA
Benzoxepin and benzothiepin derivatives as potent, orally active inhibitors of 5-lipoxygenase
TBA
Design of pyrrolo-1,4-benzoxazine derivatives as inhibitors of 5-lipoxygenase and PAF antagonists with anthihistaminic properties
TBA
1-Phenyl-[2H]-tetrahydropyridazin-3-one, A-53612, a selective orally active 5-lipoxygenase inhibitor
TBA
Phenothiazine and phenoxazine derivatives of nafazatrom. In vitro evaluation as 5-lipoxygenase and iron-dependent lipid peroxidation inhibitors.
TBA
Synthesis and 5-lipoxygenase inhibitory activity of new cinnamoyl and caffeoyl clusters.
Université
Characterization of novel furan compounds on the basis of their radical scavenging activity and cytoprotective effects against glutamate- and lipopolysaccharide-induced insults.
National Institute of Advanced Industrial Science and Technology (Aist)
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Synthesis and biological evaluation of 1-(benzenesulfonamido)-2-[5-(N-hydroxypyridin-2(1H)-one)]acetylene regioisomers: a novel class of 5-lipoxygenase inhibitors.
University of Alberta
Inhibition of leukocyte functions by the alkaloid isaindigotone from Isatis indigotica and some new synthetic derivatives.
Universidad De Murcia
Workup-dependent formation of 5-lipoxygenase inhibitory boswellic acid analogues.
Institute of Pharmaceutical Sciences
5-Lipoxygenase and cyclooxygenase-1 inhibitory active compounds from Atractylodes lancea.
Heinrich-Heine-UniversitäT DüSseldorf
Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening.
Johann Wolfgang Goethe-UniversitäT
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.
Tahitian Noni International
Substituted coumarins as potent 5-lipoxygenase inhibitors.
Merck Frosst Centre For Therapeutic Research
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues.
Pfizer
New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
Université
Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity.
Ucb Pharma
4-[5-Fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]phenyl]-3,4,5,6- tetrahydro-2H-pyran-4-carboxamide, an orally active inhibitor of 5-lipoxygenase with improved pharmacokinetic and toxicology characteristics.
Pfizer
Synthesis and activity of a new methoxytetrahydropyran derivative as dual cyclooxygenase-2/5-lipoxygenase inhibitor.
Laboratoires Innothera
Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation.
Universidade Federal Do Rio De Janeiro
Quinolines as potent 5-lipoxygenase inhibitors: synthesis and biological profile of L-746,530.
Merck Frosst Centre For Therapeutic Research
New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.
Procter & Gamble Pharmaceuticals
New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.
Procter & Gamble Pharmaceuticals
Novel indole-2-carboxamide and cycloalkeno[1,2-b]indole derivatives. Structure-activity relationships for high inhibition of human LDL peroxidation.
Université
Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Abbott Laboratories
5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.
Abbott Laboratories
Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.
Merck Frosst Centre For Therapeutic Research
Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series.
Astrazeneca
Antipsoriatic anthrones with modulated redox properties. 2. Novel derivatives of chrysarobin and isochrysarobin--antiproliferative activity and 5-lipoxygenase inhibition.
UniversitäT Regensburg
Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid.
Merck Frosst Centre For Therapeutic Research
Naphthalenic lignan lactones as selective, nonredox 5-lipoxygenase inhibitors. Synthesis and biological activity of (methoxyalkyl)thiazole and methoxytetrahydropyran hybrids.
Merck Frosst Centre For Therapeutic Research
(6,7-Diaryldihydropyrrolizin-5-yl)acetic acids, a novel class of potent dual inhibitors of both cyclooxygenase and 5-lipoxygenase.
Merckle
Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma.
Solvay Pharma
Derivatives of 2-[[N-(Aminocarbonyl)-N-hydroxyamino]methyl]-1,4- benzodioxan as orally active 5-lipoxygenase inhibitors.
Ciba-Geigy
Chiral dioxolane inhibitors of leukotriene biosynthesis: structure-activity relationships and syntheses using asymmetric dihydroxylation.
Zeneca Pharmaceuticals
Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.
Merck Frosst Centre For Therapeutic Research
Acetohydroxamic acids as potent, selective, orally active 5-lipoxygenase inhibitors.
Wellcome Research Laboratories
Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224.
Merck Frosst Canada
Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis.
Rorer Central Research
Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acryl amides.
Dainippon Pharmaceutical
Studies on hindered phenols and analogues. 2. 1,3-Benzoxathioles having SRS-A inhibiting activity.
Sankyo
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
Molecular Therapeutics
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.
Rorer Central Research
Effect of structure on potency and selectivity in 2,6-disubstituted 4-(2-arylethenyl)phenol lipoxygenase inhibitors.
Boehringer Ingelheim Pharmaceuticals
Syntheses of 5,7,8- and 5,6,7-trioxygenated 3-alkyl-3',4'-dihydroxyflavones and their inhibitory activities against arachidonate 5-lipoxygenase.
University of Tokushima
(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.
Ici Pharmaceuticals Group
Synthesis and biological evaluation of 4-imidazolylflavans as nonsteroidal aromatase inhibitors.
BiomolÉCules Et Cibles Cellulaires Tumorales