PMID

Data

Article Title

Organization

Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.

Goethe-University Frankfurt

The"Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.

St. John'S University

Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.

Setsunan University

 

A new structural analogue antagonist of peptido-leukotrienes. The discovery of bay x7195

TBA

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Development of a novel series of styrylquinoline compounds as high-affinity leukotriene D4 receptor antagonists: synthetic and structure-activity studies leading to the discovery of (+-)-3-[[[3-[2-(7-chloro-2-quinolinyl)-(E)-ethenyl]phenyl][[3- (dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic

Merck Frosst Centre For Therapeutic Research

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

Wyeth-Ayerst Research

Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists.

Universitat De Barcelona

 

THE ROLE OF ARGININE IN THE BINDING OF LTD₄ ANTAGONISTS TO cysLT₁ RECEPTORS OF GUINEA PIG LUNG

TBA

 

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

TBA

 

Discovery of MK-0476, a potent and orally active leukotriene D₄ receptor antagonist devoid of peroxisomal enxyme induction

TBA

 

Evolution of a series of non-quinoline leukotriene D₄ receptor antagonist; synthesis and sar of benzothiazoles and thiazoles substituted benzyl alcohols as potent LTD₄ antagonists

TBA

 

The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D₄ (LTD₄)/platelet activating factor (PAF) receptor antagonists.

TBA

 

LTD₄ Receptor binding activity of novel pyridine chromanols: qualitative correlation with pKa

TBA

 

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

TBA

 

The discovery of L-699,392, a novel potent and orally active leukotriene D₄ receptor antagonist

TBA

 

A new series of potent LTD₄ antagonists in the styrylquinoline class.

TBA

 

The discovery of a new structural class of potent orally active leukotriene D₄ antagonists

TBA

Derivation of pharmacophore and CoMFA models for leukotriene D(4) receptor antagonists of the quinolinyl(bridged)aryl series.

Laboratorios Menarini

Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.

Pfizer

Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.

Pfizer

N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4.

Pfizer

Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.

Novartis Pharma

Development of a three-dimensional CysLT1 (LTD4) antagonist model with an incorporated amino acid residue from the receptor.

Vrije Universiteit

Synthesis and structure-activity relationships of carboxyflavones as structurally rigid CysLT1 (LTD4) receptor antagonists.

Vrije Universiteit

Synthesis, structure-activity relationships, and pharmacological evaluation of a series of fluorinated 3-benzyl-5-indolecarboxamides: identification of 4-[[5-[((2R)-2-methyl-4,4,4-trifluorobutyl)carbamoyl]-1-methyl indol- 3-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl]benzamide, a potent, orall

Zeneca Pharmaceuticals Group

(Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.

Vrije Universiteit

Substituted 3-(phenylmethyl)-1H-indole-5-carboxamides and 1-(phenylmethyl)indole-6-carboxamides as potent, selective, orally active antagonists of the peptidoleukotrienes.

Ici Pharmaceuticals Group

Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.

TBA

High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.

TBA

Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.

TBA

3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.

Roche Research Center

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

Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles.

Ici Pharmaceuticals Group

Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.

Merck Frosst Centre For Therapeutic Research

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.

Rorer Central Research

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

Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.

Rhone-Poulenc Rorer Central Research

Peptide leukotrienes: current status of research.

Ici Pharmaceuticals Group