PMID

Data

Article Title

Organization

Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.

Goethe-University Frankfurt

Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.

Eli Lilly

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

St. John'S University

Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.

Shanghai Institute of Materia Medica

Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.

Glenmark Research Centre

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

Setsunan University

Discovery of a potent, orally available dual CysLT1 and CysLT2 antagonist with dicarboxylic acid.

Ono Pharmaceutical

Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.

Ono Pharmaceutical

 

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

TBA

Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela

Pfizer

Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.

Zhejiang University

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Modulators of leukotriene biosynthesis and receptor activation.

Abbott 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 Receptor Binding in Drug Discovery

TBA

 

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

 

Discovery of L-740,515, a potent thienopyridine cysLT₁ receptor (LTD₄ receptor) antagonist

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

Treatment of allergy: Overview of synthetic anti-allergy small molecules in medicinal chemistry.

Zhejiang Sci-Tech University

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.

University of Naples "Federico Ii

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

A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.

Merck Frosst Center For Therapeutic Research

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

The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.

Rorer Central 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

Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents.

Warner-Lambert

Splicing factor SF3b as a target of the antitumor natural product pladienolide.

Eisai

Biarylether amide quinolines as liver X receptor agonists.

Wyeth Research

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Bristol-Myers Squibb

Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.

Sunesis Pharmaceuticals

Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.

Astrazeneca