PMID

Data

Article Title

Organization

Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Jagiellonian University Medical College

Metabolism study and biological evaluation of bosentan derivatives.

University of Perugia

Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.

Jagiellonian University Medical College

Applications of Fluorine in Medicinal Chemistry.

Bristol-Myers Squibb Research and Development

Chemical synthesis of tetracyclic terpenes and evaluation of antagonistic activity on endothelin-A receptors and voltage-gated calcium channels.

Kansas State University

Discovery of phenoxybutanoic acid derivatives as potent endothelin antagonists with antihypertensive activity.

Southeast University

New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.

Zeneca Pharmaceuticals

Chemokine receptor antagonists.

National Heart and Lung Institute

The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

Actelion Pharmaceuticals

Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.

China Pharmaceutical University

Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.

H. Lundbeck

5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.

The University of Mississippi

New chlorinated diphenyl ethers from an Aspergillus species.

University of Western Australia

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.

Encysive Pharmaceuticals

Selective optimization of side activities: another way for drug discovery.

Prestwick Chemical

Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Potent and selective ET-A antagonists. 2. Discovery and evaluation of potent and water soluble N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.

Tanabe Seiyaku

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

Neogenesis

Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).

Bristol-Myers Squibb Pharmaceutical Research Institute

Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.

Rh£Ne-Poulenc Rorer

Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): examination of its pharmacokinetic and spectral properties.

Warner-Lambert

Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.

Tsukuba Research Institute

Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.

Warner-Lambert

Endothelin: a new challenge.

Warner-Lambert

Design of a functional hexapeptide antagonist of endothelin.

Warner-Lambert

Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.

Merck

 

Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan

TBA

 

Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin

TBA

 

Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide

TBA

 

Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity

TBA

 

Structure-activity relationships of monocyclic endothelin analogs

TBA

Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acids as selective ET(A) antagonists.

St. John'S University

Spiroindolones, a potent compound class for the treatment of malaria.

Swiss Tropical and Public Health Institute

A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.

Università

 

A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri

TBA

 

Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists

TBA

 

Search for surrogates: A study of endothelin receptor antagonist structure activity relationships

TBA

 

γ-Carbamate butenolide analogues as potent ET_A selective endothelin receptor antagonists and prodrugs

TBA

 

Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists

TBA

 

2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and et_A selective endothelin receptor antagonists

TBA

 

1,4-Diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as endothelin receptor antagonists

TBA

 

1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

TBA

 

Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists

TBA

 

Thiophenesulfonamides as endothelin receptor antagonists

TBA

 

Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists

TBA

 

1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists

TBA

 

The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317

TBA

 

Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors

TBA

 

Discovery of substituted 8,9-dicarboxyldibenzo [2,3:5,6] bicyclo [5.2.0] nonan-4-ones with moderate binding affinity to the endothelin ET_A and ET_B receptors

TBA

 

Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)

TBA

 

Quantitative structure-activity relationships study of endothelin-1 analogs

TBA

 

Structure-activity relationships in a series of monocyclic endothelin analogues

TBA

 

Endothelin receptor ligands. replacement net approach to SAR determination of potent hexapeptides

TBA

 

Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His¹⁶]

TBA

Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.

Covx Research

Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.

Actelion Pharmaceuticals

Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.

University of Innsbruck

Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.

Glaxosmithkline

Solid-phase synthesis of endothelin receptor antagonists.

Basf

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.

Actelion Pharmaceuticals

Bis-sulfonamides as endothelin receptor antagonists.

Actelion Pharmaceuticals

Structure-Activity relationships of 2-substituted 5,7-Diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids as a novel class of endothelin receptor antagonists.

Tsukuba Research Institute

Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure-activity relationships of a novel class of endothelin-A receptor antagonists and discovery of potent and selective receptor antagonist, 2-(benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic acid (S-1255). 1. Study on structure-activity relationships and bas

Shionogi

Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.

Bristol-Myers Squibb Pharmaceutical Research Institute

The design and synthesis of a novel series of indole derived selective ET(A) antagonists.

Pfizer

Pyridine alkaloids with activity in the central nervous system.

University of Auckland

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.

Abbott Laboratories

Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.

Tanabe Seiyaku

Isoindolines: a new series of potent and selective endothelin-A receptor antagonists.

Novartis Institute For Biomedical Research

Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.

Texas Biotechnology

Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.

Hoechst Marion Roussel

Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.

Shionogi

Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis.

Centre Hospitalier Universitaire Vaudois (Chuv)

Nonpeptide endothelin antagonists: from lower affinity pyrazol-5-ols to higher affinity pyrazole-5-carboxylic acids.

Hoechst Marion Roussel

Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.

Iowa State University

From bosentan (TracleerŪ) to macitentan (OpsumitŪ): The medicinal chemistry perspective.

Actelion Pharmaceuticals

Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.

RhôNe-Poulenc Rorer

Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.

Abbott Laboratories

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.

Abbott Laboratories

Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist.

Basf

Butenolide endothelin antagonists with improved aqueous solubility.

Warner-Lambert

Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.

Merck

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.

Shanghaitech University

Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630.

Takarazuka Research Institute

Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.

Takarazuka Research Institute

Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.

Rti International

Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.

Merck

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546).

Abbott Laboratories

Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.

RhôNe-Poulenc Rorer

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.

Abbott Laboratories

Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.

Immunopharmaceutics

Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.

Immunopharmaceutics

Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.

Warner-Lambert

Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.

Abbott Laboratories

2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.

Abbott Laboratories

Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.

Basf

Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.

Abbott Laboratories

Azole endothelin antagonists. 2. Structure-activity studies.

Abbott Laboratories

Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.

Abbott Laboratories

Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.

Janssen Pharmaceutica

The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.

Bristol-Myers Squibb Pharmaceutical Research Institute

1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.

Smithkline Beecham Pharmaceuticals

Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.

Warner-Lambert

Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.

Warner-Lambert

Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.

Tsukuba Research Institute

Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.

Phenex Pharmaceuticals

Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ET

St. John'S University

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.

Sanofi-Synthelabo Recherche

N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Pudue Pharma Discovery Research

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

Pharmacological properties of J-104132 (L-753,037), a potent, orally active, mixed ETA/ETB endothelin receptor antagonist.

Banyu Pharmaceutical

Nonpeptide endothelin receptor antagonists. XI. Pharmacological characterization of SB 234551, a high-affinity and selective nonpeptide ETA receptor antagonist.

Smithkline Beecham Pharmaceuticals

SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.

Sanofi Recherche

Affinity and selectivity of PD156707, a novel nonpeptide endothelin antagonist, for human ET(A) and ET(B) receptors.

University of Cambridge