141 articles for thisTarget
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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
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
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
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
Takeda Chemical Industries
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
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
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
Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography.
University Hospital Mu£Nster
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
PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies.
University Hospital M£Nster
A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri
TBA
Isolation and Structure Elucidation of 34-Sulfatobastadin 13, an Inhibitor of the Endothelin A Receptor, from a Marine Sponge of the Genus Ianthella
TBA
Search for surrogates: A study of endothelin receptor antagonist structure activity relationships
TBA
γ-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
TBA
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists
TBA
Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists
TBA
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
TBA
The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317
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 ETA and ETB receptors
TBA
Linear peptide ETA antagonists: rational design and practical derivatization of N-terminal amino- and imino-carbonylated tripeptide derivatives
TBA
Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)
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
Recent progress toward developing axial chirality bioactive compounds.
Shandong University
Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives.
Shanghai Institute of Materia Medica
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
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
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
Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists.
Tanabe Seiyaku
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
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 (Tracleer®) to macitentan (Opsumit®): 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
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. 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 RORγt.
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
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Duquesne University
Inhibition of the enzymatic activity of heme oxygenases by azole-based antifungal drugs.
Queen'S University
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Johnson & Johnson Pharmaceutical