PMID

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Article Title

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Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X

The University Of Sydney

Escape from adamantane: Scaffold optimization of novel P2X7 antagonists featuring complex polycycles.

Universitat De Barcelona

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.

Janssen Research And Development

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Janssen Research And Development

Promising Therapeutic Potential of P2X7 Modulators.

Therachem Research Medilab (India)

Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.

Janssen Research And Development

Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.

Janssen Research And Development

Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.

University Of Leeds

Discovery of novel 2,5-dioxoimidazolidine-based P2X(7) receptor antagonists as constrained analogues of KN62.

Gwangju Institute Of Science And Technology (Gist)

Carbamazepine derivatives with P2X4 receptor-blocking activity.

University Of Bonn

Design and synthesis of potent and selective P2X3 receptor antagonists derived from PPADS as potential pain modulators.

Gwangju Institute Of Science And Technology (Gist)

Synthesis and structure-activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists.

Gwangju Institute Of Science And Technology

Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

Janssen Research And Development

Ion channels as therapeutic targets: a drug discovery perspective.

Pfizer

Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.

Abbott Laboratories

Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.

Abbott Laboratories

Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.

Glaxosmithkline

Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.

Glaxosmithkline

Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.

Glaxosmithkline

Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.

Glaxosmithkline

Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.

Roche Palo Alto

Antagonists of the P2X(7) receptor. From lead identification to drug development.

Astrazeneca

Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.

Abbott Laboratories

Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.

Abbott Laboratories

Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.

Abbott Laboratories

Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.

Abbott Laboratories

Novel P2X7 receptor antagonists.

Astrazeneca

N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.

University Of Bonn

Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.

Gwangju Institute Of Science And Technology (Gist)

Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.

Abbott Bioresearch Center

Purine and pyrimidine (P2) receptors as drug targets.

National Institute Of Diabetes

Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.

Astrazeneca R&D Charnwood

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2.

Merck Research Laboratories

Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor.

Pfizer

Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.

Glaxosmithkline

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.

Merck Research Laboratories

Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.

Pfizer

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.

Pfizer

Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.

Institute Of Science & Technology

Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening.

University Of Sydney

Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.

Roche Palo Alto

Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.

Roche Palo Alto

Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists.

Institute Of Science And Technology (Gist)

Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.

Abbott Bioresearch Center

Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.

Institute Of Science And Technology

Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.

Astrazeneca R&D Charnwood

From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.

Università

Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.

Università

Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.

Università

Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.

Università

Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.

Gwangju Institute Of Science And Technology (Gist)

Novel Series of Dihydropyridinone P2X7 Receptor Antagonists.

Hoffmann-La Roche

Purinergic receptor P2X?: a novel target for anti-inflammatory therapy.

Punjabi University

1,4-Naphthoquinones potently inhibiting P2X7 receptor activity.

Instituto Oswaldo Cruz

Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.

Gwangju Institute Of Science And Technology (Gist)

1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.

Instituto De Tecnologia Em F£Rmacos

Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.

Shionogi

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Janssen Research And Development

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Janssen Research And Development

Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X

The University Of Sydney

In vitro pharmacological profile of SK-896, a new human motilin analogue.

Sanwa Kagaku Kenkyusho

Mu-opioid receptor specific antagonist cyprodime: characterization by in vitro radioligand and [35S]GTPgammaS binding assays.

Hungarian Academy Of Sciences

Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.

Monash University

Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.

Merck Research Laboratories

Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.

The Scripps Research Institute

NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.

India Central Drug Research Institute

SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.

Merck Research Laboratories

Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors.

Nagoya City University

Functional cloning of Bacillus anthracis dihydrofolate reductase and confirmation of natural resistance to trimethoprim.

Oklahoma State University At Stillwater

Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.

Institut Curie

The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.

Merck Research Laboratories

Structure-activity relationship studies of novel carbocyclic influenza neuraminidase inhibitors.

Gilead Sciences

Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases.

Sugen

Tyrosine kinase inhibitors. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding.

University Of Auckland

 

SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C.

Sphinx Laboratories