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Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.

China Pharmaceutical University

Development and evaluation of ST-1829 based on 5-benzylidene-2-phenylthiazolones as promising agent for anti-leukotriene therapy.

Goethe-University Frankfurt

Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.

Ici Pharmaceuticals Group

 

Cyclic aryl hydroxamic acids: synthesis and inhibition of 5-lipoxygenase

TBA

Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.

Peking University

Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.

Abbott Laboratories

1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.

Smithkline Beecham Pharmaceuticals

Novel dual inhibitors of 5-lipoxygenase and thromboxane A2 synthetase: synthesis and structure-activity relationships of 3-pyridylmethyl-substituted 2-amino-6-hydroxybenzothiazole derivatives.

Eisai

Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.

Warner-Lambert

Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.

Warner-Lambert

5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.

Wyeth-Ayerst Research

1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.

Pfizer

2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity.

E.I. Du Pont De Nemours

4-Hydroxy-3-quinolinecarboxamides with antiarthritic and analgesic activities.

Centre De Recherches Roussel-Uclaf

Synthesis and 5-lipoxygenase inhibitory activity of 5-hydroperoxy-6,8,11,14-eicosatetraenoic acid analogues.

TBA

Hydroxamic acid inhibitors of 5-lipoxygenase.

TBA

Structural requirements for the inhibition of 5-lipoxygenase by 15-hydroxyeicosa-5,8,11,13-tetraenoic acid analogues.

TBA

Novel 1H-benzimidazol-4-ols with potent 5-lipoxygenase inhibitory activity.

Beecham Pharmaceuticals Research Division

 

Antiinflammatory -benzeneethanamines. III

TBA

 

Topical antiinflammatory dehydroabietylamine derivatives. IV

TBA

 

O-alkylcarboxylate oxime and N-hydroxyurea analogs of substituted indole leukotriene biosynthesis inhibitors

TBA

 

Catechol based inhibitors of 15-lipoxygenase

TBA

 

Cmi-206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor

TBA

 

Synthesis and pharmacological profile of two novel heterocyclic chromanols, CP-80,798 and CP-85,958, as potent LTD₄ receptor antagonists

TBA

 

2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis

TBA

 

A novel series of highly potent 5-lipoxygenase inhibitors; 2-aryldienylbenzoxazoles

TBA

 

Design of pyrrolo-1,4-benzoxazine derivatives as inhibitors of 5-lipoxygenase and PAF antagonists with anthihistaminic properties

TBA

 

4-[5-(2,3-dihydroxyphenyl)pentyloxy]-2-hydroxy-3-propylbenzoic acid (Ro 24-0553): an orally active 5-lipoxygenase inhibitor with antiinflammatory activity

TBA

 

Cyclooxygenase and 5-lipoxygenase inhibitory activity of 2,6 di-t-butylphenols linked by a sulfur atom to 1,3,4-thiadiazoles and 1,3,4-oxadiazoles

TBA

 

Vinylogous hydroxamic acids: 5-lipoxygenase inhibitors

TBA

 

Synthesis and cyclooxygenase and 5-lipoxygenase inhibitory activity of some thiazolidene-4-one analogs of meclofenamic acid

TBA

 

Development of L-689,065 - the prototype of a new class of potent 5-lipoxygenase inhibitors

TBA

 

Synthesis of reversed hydroxamic acids of indomethacin: dual inhibitors of cyclooxygenase and 5-lipoxygenase

TBA

 

1-Phenyl-[2H]-tetrahydropyridazin-3-one, A-53612, a selective orally active 5-lipoxygenase inhibitor

TBA

 

Structural analysis of 2-aryl-1,3-dione compounds as inhibitors of 5-lipoxygenase

TBA

 

Conversion of NSAIDS into balanced dual inhibitors of cyclooxygenase and 5-lipoxygenase

TBA

Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.

Peking Union Medical College And Chinese Academy Of Medical Sciences

Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.

Chinese Academy Of Sciences

5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.

Ucb Pharma

N-Aminoindoline derivatives as inhibitors of 5-lipoxygenase.

Université

5-Lipoxygenase as a drug target: A review on trends in inhibitors structural design, SAR and mechanism based approach.

School Of Advanced Sciences

N-hydroxyurea and hydroxamic acid inhibitors of cyclooxygenase and 5-lipoxygenase.

The R. W. Johnson Pharmaceutical Research Institute

Design, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents.

Nanjing University

(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.

University Of Virginia

New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.

Procter & Gamble Pharmaceuticals

Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.

Oxis International

Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.

Abbott Laboratories

Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea.

Smithkline Beecham Pharmaceuticals

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

(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.

Smithkline Beecham Pharmaceuticals

Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity.

Hoechst-Roussel Pharmaceuticals

1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities.

Warner-Lambert

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

Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.

Warner-Lambert

3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors.

Tokushima Bunri University

Antiinflammatory 4,5-diarylpyrroles: synthesis and QSAR.

Dupont Pharmaceuticals

Synthesis and 5-lipoxygenase inhibitory activities of some novel 2-substituted 5-benzofuran hydroxamic acids.

R. W. Johnson Pharmaceutical Research Institute

Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.

Wyeth Research (U.K.)

Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.

TBA

Syntheses of 5,6,7- and 5,7,8-trioxygenated 3',4'-dihydroxyflavones having alkoxy groups and their inhibitory activities against arachidonate 5-lipoxygenase.

TBA

In vivo characterization of hydroxamic acid inhibitors of 5-lipoxygenase.

Abbott Laboratories

Benzopyrroloxazines containing a bridgehead nitrogen atom as promising scaffolds for the achievement of biologically active agents.

University Of Calabria

Orally active hydroxamic acid inhibitors of leukotriene biosynthesis.

Abbott Laboratories

Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.

Abbott Laboratories

Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.

TBA

Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.

University Of Pennsylvania

Synthesis and antiallergic activity of a novel series of 5-lipoxygenase inhibitors.

TBA

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

N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.

Wyeth-Ayerst Research

Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.

Molecular Therapeutics

Hydroxamic acid inhibitors of 5-lipoxygenase: quantitative structure-activity relationships.

Abbott Laboratories

Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.

Centre De Recherches De Vitry

Synthesis of novel hybrids of pyrazole and coumarin as dual inhibitors of COX-2 and 5-LOX.

Nanjing University

Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.

Warner-Lambert

N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.

Wyeth-Ayerst Research

4-hydroxythiazole inhibitors of 5-lipoxygenase.

Abbott Laboratories

Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase.

Institute For Bio-Medical Research

Dual inhibitors of thromboxane A2 synthase and 5-lipoxygenase with scavenging activity of active oxygen species. Synthesis of a novel series of (3-pyridylmethyl)benzoquinone derivatives.

Takeda Chemical Industries

5-Lipoxygenase inhibitors: the synthesis and structure-activity relationships of a series of 1-phenyl-3-pyrazolidinones.

Sterling Research Group

Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.

Warner-Lambert

(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.

Ici Pharmaceuticals Group

Novel 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols with topical antiinflammatory activity.

Dupont Pharmaceuticals

Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis.

Dupont Pharmaceuticals

Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase.

Merck Frosst Centre For Therapeutic Research