| Title : Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists - Carroll_2007_Bioorg.Med.Chem.Lett_17_4044 |
| Author(s) : Carroll WA , Kalvin DM , Perez Medrano A , Florjancic AS , Wang Y , Donnelly-Roberts D , Namovic MT , Grayson G , Honore P , Jarvis MF |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :4044 , 2007 |
|
Abstract :
Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X(7) antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain. |
| PubMedSearch : Carroll_2007_Bioorg.Med.Chem.Lett_17_4044 |
| PubMedID: 17482819 |
Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts D, Namovic MT, Grayson G, Honore P, Jarvis MF (2007)
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists
Bioorganic & Medicinal Chemistry Lett
17 :4044
Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts D, Namovic MT, Grayson G, Honore P, Jarvis MF (2007)
Bioorganic & Medicinal Chemistry Lett
17 :4044