| Title : Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists - Morytko_2008_Bioorg.Med.Chem.Lett_18_2093 |
| Author(s) : Morytko MJ , Betschmann P , Woller K , Ericsson A , Chen H , Donnelly-Roberts D , Namovic MT , Jarvis MF , Carroll WA , Rafferty P |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :2093 , 2008 |
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Abstract :
A novel series of cyanoguanidine-piperazine P2X(7) antagonists was designed based upon the structure of A-740003. Structure-activity relationship (SAR) studies focused on the piperazine moiety and the right hand side substitution. Compounds were assayed for activity at human and rat P2X(7) receptors and compound 29 was found to possess potent activity (IC(50)=30-60 nM) at both species. |
| PubMedSearch : Morytko_2008_Bioorg.Med.Chem.Lett_18_2093 |
| PubMedID: 18272365 |
Morytko MJ, Betschmann P, Woller K, Ericsson A, Chen H, Donnelly-Roberts D, Namovic MT, Jarvis MF, Carroll WA, Rafferty P (2008)
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists
Bioorganic & Medicinal Chemistry Lett
18 :2093
Morytko MJ, Betschmann P, Woller K, Ericsson A, Chen H, Donnelly-Roberts D, Namovic MT, Jarvis MF, Carroll WA, Rafferty P (2008)
Bioorganic & Medicinal Chemistry Lett
18 :2093