PMID

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Article Title

Organization

o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists.

Eli Lilly

trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.

Pfizer

Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.

Neogenesis

Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase.

Eisai

Modulators of leukotriene biosynthesis and receptor activation.

Abbott Laboratories

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

Synthesis of structural analogs of leukotriene B4 and their receptor binding activity.

Smithkline Beecham Pharmaceuticals

 

Synthesis and pharmacologic activity of hydroxyacetophenone-substituted benzophenone/xanthone leukotriene B4 receptor antagonists

TBA

Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1.

Roche Research Center

The Role of Receptor Binding in Drug Discovery

TBA

New Leukotriene B₄ Receptor Antagonist: Leucettamine A and Related Imidazole Alkaloids from the Marine Sponge Leucetta microraphis

TBA

 

N-aryl cinnamides: A novel class of rigid and highly potent leukotriene B₄ receptor antagonists

TBA

 

3-Amino-1,2-benzisoxazoles: A new family of potent inhibitors of LTB₄ binding to the human neutrophils

TBA

 

Synthesis and pharmacological profile of new 1,3-disubstituted cyclohexanes as leukotriene B₄ receptor antagonists

TBA

 

Synthesis and in vitro profile of 7-substituted quinoline chromanols as novel, non-acidic LTB₄ antagonists

TBA

 

2-alkyl-4-ethyl-5-[6-methyl-6-(2H-tetrazol-5-yl)heptyloxy]phenol leukotriene B₄ receptor antagonists

TBA

 

Synthesis and pharmacological activity of SC-53228, a leukotriene B₄ receptor antagonist with high intrinsic potency and selectivity

TBA

 

Structural analogues of LY292728, a highly potent xanthone dicarboxylic acid leukotriene B₄ receptor antagonist: spatial positioning of the secondary acid group

TBA

 

Acid unit modifications of 1,2,4,5-substituted hydroxyacetophenones and the effect on in vitro and in vivo LTB₄ receptor antagonism

TBA

 

Ortho-alkoxyphenol leukotriene B4 receptor antagonists: effect of a chroman carboxylic acid.

TBA

 

Ortho-alkoxyphenol leukotriene B4 receptor antagonists

TBA

 

Enantioselective total synthesis and pharmacologic profile of 12-deoxy-12(S)-methyl leukotriene B₄

TBA

Synthesis of leukotriene B4 antagonists labeled with In-111 or Tc-99m to image infectious and inflammatory foci.

Bristol-Myers Squibb Medical Imaging

Structure-activity relationships of indole cytosolic phospholipase A(2)alpha inhibitors: substrate mimetics.

Wyeth Research

Leukotriene B4 photoaffinity probes: design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes.

Upresa-Cnrs 5074

Carboxy-substituted cinnamides: a novel series of potent, orally active LTB4 receptor antagonists.

Novartis Pharmaceuticals

(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

Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain.

RhôNe-Poulenc Rorer

A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships.

Rhone-Poulenc Rorer Central Research

(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.

Smithkline Beecham Pharmaceuticals

Design, synthesis, and pharmacological evaluation of potent xanthone dicarboxylic acid leukotriene B4 receptor antagonists.

Eli Lilly

Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.

Eli Lilly

Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues.

Smithkline Beecham Pharmaceuticals

Trisubstituted pyridine leukotriene B4 receptor antagonists: synthesis and structure-activity relationships.

Smithkline Beecham Pharmaceuticals

Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles.

Eli Lilly

(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.

Smithkline Beecham Pharmaceuticals

(+)-1-(3S,4R)-[3-(4-phenylbenzyl)-4-hydroxychroman-7-yl]cyclopentane carboxylic acid, a highly potent, selective leukotriene B4 antagonist with oral activity in the murine collagen-induced arthritis model.

Pfizer

Second-generation leukotriene B4 receptor antagonists related to SC-41930: heterocyclic replacement of the methyl ketone pharmacophore.

Searle Research And Development

Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.

Eli Lilly

7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist.

G.D. Searle And

Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.

Eli Lilly

omega-[(4,6-Diphenyl-2-pyridyl)oxy]alkanoic acid derivatives: a new family of potent and orally active LTB4 antagonists.

Centre De Recherche De Vitry-Alfortville

omega-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists.

Centre De Recherche De Vitry-Alfortville

4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.

Rhone-Poulenc Rorer Central Research

Omega-[(omega-arylalkyl)thienyl]alkanoic acids: from specific LTA4 hydrolase inhibitors to LTB4 receptor antagonists.

Centre De Recherche De Vitry-Alfortville

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