The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28279849 |
38 |
Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X |
The University of Sydney |
| 28126517 |
7 |
Escape from adamantane: Scaffold optimization of novel P2X7 antagonists featuring complex polycycles. |
Universitat De Barcelona |
| 27595421 |
21 |
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 |
| 27548392 |
76 |
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 |
| 27096039 |
20 |
Promising Therapeutic Potential of P2X7 Modulators. |
Therachem Research Medilab (India) |
| 26707399 |
45 |
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 |
| 26099534 |
72 |
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 |
| 26099538 |
8 |
Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human. |
University of Leeds |
| 25597334 |
67 |
Discovery of novel 2,5-dioxoimidazolidine-based P2X(7) receptor antagonists as constrained analogues of KN62. |
Gwangju Institute of Science and Technology (Gist) |
| 24411477 |
84 |
Carbamazepine derivatives with P2X4 receptor-blocking activity. |
University of Bonn |
| 24246730 |
34 |
Design and synthesis of potent and selective P2X3 receptor antagonists derived from PPADS as potential pain modulators. |
Gwangju Institute of Science and Technology (Gist) |
| 24900736 |
1 |
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release. |
University of Cambridge |
| 23510563 |
9 |
Synthesis and structure-activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists. |
Gwangju Institute of Science and Technology |
| 24900687 |
3 |
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists. |
Janssen Research and Development |
| 23121096 |
86 |
Ion channels as therapeutic targets: a drug discovery perspective. |
Pfizer |
| 17482819 |
36 |
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists. |
Abbott Laboratories |
| 21536435 |
90 |
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists. |
Abbott Laboratories |
| 20934331 |
23 |
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor. |
Glaxosmithkline |
| 20673717 |
30 |
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. |
Glaxosmithkline |
| 20579878 |
26 |
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor. |
Glaxosmithkline |
| 20399651 |
34 |
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor. |
Glaxosmithkline |
| 20045645 |
66 |
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist. |
Roche Palo Alto |
| 19191585 |
143 |
Antagonists of the P2X(7) receptor. From lead identification to drug development. |
Astrazeneca |
| 19397270 |
122 |
Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain. |
Abbott Laboratories |
| 18438986 |
71 |
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists. |
Abbott Laboratories |
| 18272366 |
74 |
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 |
| 16759108 |
40 |
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. |
Abbott Laboratories |
| 14592504 |
23 |
Novel P2X7 receptor antagonists. |
Astrazeneca |
| 23075067 |
98 |
N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists. |
University of Bonn |
| 22400713 |
39 |
Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists. |
Gwangju Institute of Science and Technology (Gist) |
| 21207957 |
163 |
Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor. |
University of Bonn |
| 18272365 |
57 |
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists. |
Abbott Bioresearch Center |
| 12213051 |
207 |
Purine and pyrimidine (P2) receptors as drug targets. |
National Institute of Diabetes |
| 14592505 |
7 |
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists. |
Astrazeneca R&D Charnwood |
| 22078214 |
29 |
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2. |
Merck Research Laboratories |
| 21782426 |
42 |
Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor. |
Pfizer |
| 21634377 |
73 |
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. |
Amgen |
| 20634071 |
41 |
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists. |
Glaxosmithkline |
| 21570840 |
44 |
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1. |
Merck Research Laboratories |
| 21565499 |
32 |
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 |
| 20392639 |
18 |
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 |
| 19800793 |
15 |
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists. |
Institute of Science & Technology |
| 19540765 |
10 |
Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening. |
University of Sydney |
| 19231180 |
81 |
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 |
| 19231178 |
61 |
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 |
| 19110420 |
23 |
Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists. |
Institute of Science and Technology (Gist) |
| 18595695 |
43 |
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists. |
Abbott Bioresearch Center |
| 18078749 |
22 |
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor. |
Institute of Science and Technology |
| 17963373 |
36 |
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors. |
Astrazeneca R&D Charnwood |
| 17585854 |
42 |
From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor. |
Università |
| 15482953 |
2 |
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 |
| 12672232 |
28 |
Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor. |
Università |
| 31525963 |
42 |
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease. |
Universit£ |
| 32345019 |
134 |
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists. |
University of Bonn |
| 27427902 |
93 |
Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion. |
Gwangju Institute of Science and Technology (Gist) |
| 30996785 |
44 |
Investigation on 2',3'- |
University of Camerino |
| 27426304 |
76 |
The evolution of P2X7 antagonists with a focus on CNS indications. |
Janssen Pharmaceutical Research & Development |
| 30728111 |
81 |
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds. |
Shionogi |
| 10762053 |
2 |
Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor. |
Università |
| 31532206 |
26 |
Development of High-Throughput Fluorescent-Based Screens to Accelerate Discovery of P2X Inhibitors from Animal Venoms. |
University of East Anglia |
| 30528164 |
4 |
8-Hydroxy-2-(1H-1,2,3-triazol-1-yl)-1,4-naphtoquinone derivatives inhibited P2X7 Receptor-Induced dye uptake into murine Macrophages. |
Fluminense Federal University |
| 31031055 |
53 |
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists. |
Emd Serono Research and Development Institute |
| 31005444 |
8 |
Synthesis and in vitro biological evaluation of new P2X7R radioligands [ |
Indiana University School of Medicine |
| 31746599 |
78 |
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor |
Bayer |
| 26547056 |
36 |
Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists. |
Gwangju Institute of Science and Technology (Gist) |
| 26460788 |
45 |
Novel Series of Dihydropyridinone P2X7 Receptor Antagonists. |
Hoffmann-La Roche |
| 24314880 |
60 |
Purinergic receptor P2X?: a novel target for anti-inflammatory therapy. |
Punjabi University |
| 29133043 |
16 |
1,4-Naphthoquinones potently inhibiting P2X7 receptor activity. |
Instituto Oswaldo Cruz |
| 29649742 |
55 |
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) |
| 28858765 |
42 |
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 |
| 29805055 |
40 |
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 |
| 28493698 |
56 |
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 |
| 29211470 |
64 |
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 |
| 28408229 |
10 |
Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X |
The University of Sydney |
| 26123174 |
9 |
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists. |
Gwangju Institute of Science and Technology |
| 11111828 |
16 |
Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications. |
Biocentre Niederursel |
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