The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27876250 |
60 |
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 |
27318985 |
8 |
Metabolism study and biological evaluation of bosentan derivatives. |
University Of Perugia |
26988801 |
55 |
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 |
24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
22862294 |
118 |
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 |
16220969 |
219 |
Designed multiple ligands. An emerging drug discovery paradigm. |
Organon Laboratories |
15055997 |
42 |
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 |
14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
12502366 |
82 |
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 |
11585442 |
20 |
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 |
9857090 |
158 |
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 |
8691426 |
114 |
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 |
1315867 |
31 |
Endothelin: a new challenge. |
Warner-Lambert |
1317926 |
9 |
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications. |
TBA |
| 49 |
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan |
TBA |
| 20 |
Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity |
TBA |
20932745 |
26 |
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 |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical And Public Health Institute |
| 10 |
A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri |
TBA |
| 47 |
Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists |
TBA |
| 26 |
Search for surrogates: A study of endothelin receptor antagonist structure activity relationships |
TBA |
| 24 |
γ-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs |
TBA |
| 47 |
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists |
TBA |
| 26 |
1,4-Diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as endothelin receptor antagonists |
TBA |
| 55 |
1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists |
TBA |
| 61 |
Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists |
TBA |
| 52 |
Thiophenesulfonamides as endothelin receptor antagonists |
TBA |
| 138 |
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists |
TBA |
| 57 |
1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists |
TBA |
| 24 |
Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors |
TBA |
| 30 |
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 |
| 24 |
Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III) |
TBA |
17055724 |
14 |
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies. |
Covx Research |
16722631 |
87 |
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
Predix Pharmaceuticals |
15139756 |
221 |
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists. |
Actelion Pharmaceuticals |
15139753 |
55 |
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists. |
University Of Innsbruck |
15006391 |
50 |
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 |
12729650 |
2 |
Solid-phase synthesis of endothelin receptor antagonists. |
Basf |
12617929 |
114 |
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists. |
Actelion Pharmaceuticals |
12617928 |
68 |
Bis-sulfonamides as endothelin receptor antagonists. |
Actelion Pharmaceuticals |
12372497 |
40 |
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 |
12190306 |
14 |
Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
11985472 |
185 |
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 |
11844662 |
34 |
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
11755336 |
43 |
The design and synthesis of a novel series of indole derived selective ET(A) antagonists. |
Pfizer |
11689084 |
47 |
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists. |
Abbott Laboratories |
11585441 |
70 |
Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives. |
Tanabe Seiyaku |
11425549 |
30 |
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists. |
Novartis Institute For Biomedical Research |
10956219 |
26 |
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 |
10853654 |
18 |
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2. |
Iowa State University |
10479299 |
55 |
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 |
10479298 |
60 |
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity. |
Abbott Laboratories |
10447946 |
48 |
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 |
10377221 |
44 |
Butenolide endothelin antagonists with improved aqueous solubility. |
Warner-Lambert |
10098676 |
52 |
Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists. |
Merck |
9873522 |
8 |
Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630. |
Takarazuka Research Institute |
9873521 |
52 |
Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity. |
Takarazuka Research Institute |
9871621 |
26 |
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster. |
Merck |
9703472 |
112 |
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546). |
Abbott Laboratories |
9379441 |
100 |
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists. |
Abbott Laboratories |
9171878 |
69 |
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. |
Immunopharmaceutics |
9171877 |
92 |
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists. |
Immunopharmaceutics |
9089328 |
170 |
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
Warner-Lambert |
8676339 |
143 |
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. |
Abbott Laboratories |
8667356 |
50 |
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. |
Basf |
8632421 |
32 |
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption. |
Abbott Laboratories |
8201588 |
14 |
1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists. |
Smithkline Beecham Pharmaceuticals |
7731010 |
56 |
Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. |
Warner-Lambert |
7636842 |
155 |
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 |
7473559 |
85 |
Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists. |
Tsukuba Research Institute |
26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
25951978 |
38 |
Syntheses, cholinesterases inhibition, and molecular docking studies of pyrido[2,3-b]pyrazine derivatives. |
University Of Karachi |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University Of Leipzig |