The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28523109 |
79 |
Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. |
Glaxosmithkline |
| 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 |
| 27298001 |
14 |
Development of novel NK3 receptor antagonists with reduced environmental impact. |
Kyoto University |
| 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 |
| 26191358 |
105 |
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II). |
Euroscreen |
| 25738882 |
210 |
Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I). |
Euroscreen |
| 25247671 |
30 |
Development of novel neurokinin 3 receptor (NK3R) selective agonists with resistance to proteolytic degradation. |
Kyoto University |
| 24900878 |
40 |
Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists. |
Universit£ |
| 24374277 |
41 |
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists. |
Universit£ |
| 23808489 |
11 |
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways. |
Merck Research Laboratories |
| 23582449 |
20 |
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
Institute Of Organic Synthesis |
| 23466604 |
36 |
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
Universit£ |
| 23477943 |
51 |
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression. |
Bristol-Myers Squibb |
| 23473945 |
77 |
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists. |
Kyoto University |
| 22056747 |
23 |
3D-Quantitative structure-activity relationship and docking studies of the tachykinin NK3 receptor. |
Northeast Ohio Medical University |
| 21974957 |
27 |
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia. |
Glaxosmithkline |
| 19117759 |
17 |
New quinoline NK3 receptor antagonists with CNS activity. |
Neuroscience Cedd Glaxosmithkline Research & Development |
| 22574973 |
36 |
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists. |
F. Hoffmann-La Roche |
| 20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
| 16950620 |
36 |
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists. |
Merck Sharp & Dohme Research Laboratories |
| 12190319 |
15 |
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity. |
Astrazeneca Pharmaceuticals |
| 10090788 |
75 |
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412). |
Smithkline Beecham |
| 8648606 |
72 |
Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists. |
Cambridge University Forvie Site |
| 8691422 |
25 |
2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. |
Smithkline Beecham |
| 11591520 |
6 |
Discovery of novel, orally active dual NK1/NK2 antagonists. |
Astrazeneca Pharmaceuticals |
| 9871763 |
35 |
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template. |
Merck Sharp Laboratory |
| | 66 |
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds |
TBA |
| | 8 |
2,3-Substituted 2-azanorbornanes as polar -turn mimetics |
TBA |
| | 22 |
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists |
TBA |
| | 9 |
The design of polar -turn dipeptide mimetics |
TBA |
| | 24 |
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design |
TBA |
| 21376585 |
120 |
Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor. |
Euroscreen |
| 21320776 |
40 |
Synthesis and SAR of sulfoxide substituted carboxyquinolines as NK3 receptor antagonists. |
Astrazeneca Pharmaceuticals |
| 21292483 |
67 |
Identification of a new series of non-peptidic NK3 receptor antagonists. |
H. Lundbeck |
| 21047106 |
39 |
Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor. |
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy |
| 20850972 |
11 |
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists. |
F. Hoffmann-La Roche |
| 20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
| 20430616 |
36 |
Discovery of potent, balanced and orally active dual NK1/NK3 receptor ligands. |
F. Hoffmann-La Roche |
| 19817444 |
45 |
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures. |
F. Hoffmann-La Roche |
| | 1 |
A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist |
TBA |
| | 48 |
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist |
TBA |
| | 17 |
Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution |
TBA |
| | 7 |
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes |
TBA |
| | 2 |
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening. |
TBA |
| 19354254 |
24 |
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. |
Merck Research Laboratories |
| 18547807 |
19 |
Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists. |
Schering-Plough Research Institute |
| 17637506 |
33 |
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine. |
Merck |
| 16950617 |
50 |
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II. |
Merck Sharp & Dohme Research Laboratories |
| 16698264 |
37 |
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists. |
Merck Research Laboratories |
| 16682196 |
19 |
Cyclobutane derivatives as potent NK1 selective antagonists. |
Schering-Plough Research Institute |
| 14736234 |
11 |
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties. |
Astrazeneca Pharmaceuticals |
| 12161132 |
102 |
Preparation of oxime dual NK(1)/NK(2) antagonists with reduced NK(3) affinity. |
Schering-Plough Research Institute |
| 11784148 |
81 |
Novel spiropiperidines as highly potent and subtype selective sigma-receptor ligands. Part 1. |
Pharmazeutisches Institut Der UniversitäT Freiburg |
| 11356103 |
61 |
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists. |
Smithkline Beecham Pharmaceuticals |
| 9871627 |
20 |
High affinity phenylglycinol-based NK1 receptor antagonists. |
Merck Sharp And Dohme Research Laboratories |
| 9191956 |
51 |
Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. |
Smithkline Beecham S.P.A. Milano |
| 8627597 |
17 |
2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist. |
Merck Research Laboratories |
| 7518522 |
12 |
Comparison of the conformation of active and nonactive backbone cyclic analogs of substance P as a tool to elucidate features of the bioactive conformation: NMR and molecular dynamics in DMSO and water. |
Technische UniversitäT MüNchen |
| 7513763 |
92 |
Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. |
Merck Sharp And Dohme Research Laboratories |
| 23031230 |
5 |
Optimization of a direct spectrophotometric method to investigate the kinetics and inhibition of sialidases. |
Universit?? Degli Studi Di Siena |
| 24187139 |
9 |
Defining the communication between agonist and coactivator binding in the retinoid X receptor a ligand binding domain. |
University Of Alabama At Birmingham |
| 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 |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University Of Leipzig |
| 17064063 |
18 |
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Abbott Laboratories |
| 10891109 |
19 |
Docking-based development of purine-like inhibitors of cyclin-dependent kinase-2. |
Palacky University |
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