Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3297-3300
2011
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3297-3300
- Ort / Verlag
- England
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Synthesis and biological evaluation of a novel class of substituted N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine derivatives resulted in the identification of potent P2X(7) antagonists. These compounds were assayed for activity at both the human and rat P2X(7) receptors. On the benzyl moiety, a variety of functional groups were tolerated, including both electron-withdrawing and electron-donating substituents. Ortho-substitution on the benzyl group provided the greatest potency. The ortho-substituted analogs showed approximately 2.5-fold greater potency at human compared to rat P2X(7) receptors. Compounds 12 and 38 displayed hP2X(7)pIC(50)s>7.8 with less than 2-fold difference in potency at the rP2X(7).
- Sprache
- Englisch
- Identifikatoren
- eISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.04.024Titel-ID: cdi_proquest_miscellaneous_868026228
- Format
- –
- Schlagworte
- Amines - chemical synthesis, Amines - chemistry, Amines - pharmacology, Animals, Humans, Inhibitory Concentration 50, Molecular Structure, Protein Binding - drug effects, Purinergic P2X Receptor Antagonists - chemical synthesis, Purinergic P2X Receptor Antagonists - chemistry, Purinergic P2X Receptor Antagonists - pharmacology, Rats, Structure-Activity Relationship, Tetrazoles - chemical synthesis, Tetrazoles - chemistry, Tetrazoles - pharmacology