| Title : Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists - Perez-Medrano_2011_Bioorg.Med.Chem.Lett_21_3297 |
| Author(s) : Perez-Medrano A , Donnelly-Roberts D , Florjancic AS , Nelson DW , Li T , Namovic MT , Peddi S , Faltynek CR , Jarvis MF , Carroll WA |
| Ref : Bioorganic & Medicinal Chemistry Lett , 21 :3297 , 2011 |
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Abstract :
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). |
| PubMedSearch : Perez-Medrano_2011_Bioorg.Med.Chem.Lett_21_3297 |
| PubMedID: 21536435 |
Perez-Medrano A, Donnelly-Roberts D, Florjancic AS, Nelson DW, Li T, Namovic MT, Peddi S, Faltynek CR, Jarvis MF, Carroll WA (2011)
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists
Bioorganic & Medicinal Chemistry Lett
21 :3297
Perez-Medrano A, Donnelly-Roberts D, Florjancic AS, Nelson DW, Li T, Namovic MT, Peddi S, Faltynek CR, Jarvis MF, Carroll WA (2011)
Bioorganic & Medicinal Chemistry Lett
21 :3297