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 |
| 26200936 |
39 |
Applications of Fluorine in Medicinal Chemistry. |
Bristol-Myers Squibb Research and Development |
| 9083490 |
37 |
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 |
| 22931505 |
69 |
Chemokine receptor antagonists. |
National Heart and Lung Institute |
| 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 |
| 22750010 |
30 |
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 |
| 20684563 |
176 |
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 |
| 19916528 |
3 |
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 |
| 17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
| 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 |
| 10821712 |
18 |
Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity. |
Neogenesis |
| 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 |
| 9216842 |
28 |
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 |
| 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 |
| 8410970 |
106 |
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists. |
Warner-Lambert |
| 1324321 |
20 |
Design of a functional hexapeptide antagonist of endothelin. |
Warner-Lambert |
| | 49 |
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan |
TBA |
| | 28 |
Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin |
TBA |
| | 21 |
Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide |
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 |
| 20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
| | 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 |
| | 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 |
| | 15 |
The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317 |
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 |
| | 25 |
Structure-activity relationships in a series of monocyclic endothelin analogues |
TBA |
| | 18 |
Endothelin receptor ligands. replacement net approach to SAR determination of potent hexapeptides |
TBA |
| | 28 |
Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[16–21, D-His16] |
TBA |
| 17055724 |
14 |
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies. |
Covx Research |
| 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 |
| 12852756 |
5 |
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs. |
Glaxosmithkline |
| 12729650 |
2 |
Solid-phase synthesis of endothelin receptor antagonists. |
Basf |
| 12643919 |
50 |
Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
| 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 |
| 11425549 |
30 |
Isoindolines: a new series of potent and selective endothelin-A receptor antagonists. |
Novartis Institute For Biomedical Research |
| 11312921 |
16 |
Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist. |
Texas Biotechnology |
| 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 |
| 27266371 |
13 |
Endothelin-Receptor Antagonists beyond Pulmonary Arterial Hypertension: Cancer and Fibrosis. |
Centre Hospitalier Universitaire Vaudois (Chuv) |
| 10853654 |
18 |
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2. |
Iowa State University |
| 27321813 |
286 |
From bosentan (TracleerŪ) to macitentan (OpsumitŪ): The medicinal chemistry perspective. |
Actelion Pharmaceuticals |
| 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 |
| 29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
| 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 |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 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 |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 8308857 |
19 |
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 |
| 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 |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 28462837 |
48 |
Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ET |
St. John'S University |
| 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 |
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