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Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor
Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.5080-5084
2010

Details

Autor(en) / Beteiligte
Titel
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor
Ist Teil von
  • Bioorganic & medicinal chemistry letters, 2010-09, Vol.20 (17), p.5080-5084
Ort / Verlag
Amsterdam: Elsevier
Erscheinungsjahr
2010
Link zum Volltext
Quelle
MEDLINE
Beschreibungen/Notizen
  • A computational lead-hopping exercise identified compound 4 as a structurally distinct P2X(7) receptor antagonist. Structure-activity relationships (SAR) of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was identified as a potent P2X(7) antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.
Sprache
Englisch
Identifikatoren
ISSN: 0960-894X
eISSN: 1464-3405
DOI: 10.1016/j.bmcl.2010.07.033
Titel-ID: cdi_proquest_miscellaneous_748974679
Format
–
Schlagworte
Amides - chemistry, Amides - pharmacology, Biological and medical sciences, Drug Discovery, Medical sciences, Models, Molecular, Neuropharmacology, Neurotransmitters. Neurotransmission. Receptors, Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems, Pharmacology. Drug treatments, Purinergic P2 Receptor Antagonists - chemistry, Purinergic P2 Receptor Antagonists - pharmacology, Pyrrolidonecarboxylic Acid - chemistry, Receptors, Purinergic P2X7 - drug effects, Structure-Activity Relationship

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