| Title : 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 - Florjancic_2008_Bioorg.Med.Chem.Lett_18_2089 |
| Author(s) : Florjancic AS , Peddi S , Perez-Medrano A , Li B , Namovic MT , Grayson G , Donnelly-Roberts D , Jarvis MF , Carroll WA |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :2089 , 2008 |
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Abstract :
A novel series of aminotriazole-based P2X(7) antagonists was synthesized, and their structure-activity relationships (SAR) were investigated for activity at both human and rat P2X(7) receptors. Most compounds showed greater potency at the human receptor although several analogs were discovered with potent activity (pIC(50) > or = 7.5) at both human and rat P2X(7). |
| PubMedSearch : Florjancic_2008_Bioorg.Med.Chem.Lett_18_2089 |
| PubMedID: 18272366 |
Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts D, Jarvis MF, Carroll WA (2008)
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
Bioorganic & Medicinal Chemistry Lett
18 :2089
Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts D, Jarvis MF, Carroll WA (2008)
Bioorganic & Medicinal Chemistry Lett
18 :2089