| Title : Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors - Murineddu_2008_Bioorg.Med.Chem.Lett_18_6147 |
| Author(s) : Murineddu G , Murruzzu C , Curzu MM , Chelucci G , Gotti C , Gaimarri A , Legnani L , Toma L , Pinna GA |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :6147 , 2008 |
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Abstract :
Alpha series of novel 3,6-diazabicyclo[3.1.1]heptane derivatives 4a-f was synthesized and their affinity and selectivity towards alpha4beta2 and alpha7 nAChR subtypes were evaluated. The results of the current study revealed a number of compounds (4a, 4b and 4c) having a very high affinity for alpha4beta2 (K(i) at alpha4beta2 ranging from 0.023 to 0.056 nM) versus alpha7 nAChR subtypes; among these compounds, the 3-(6-bromopyridin-3-yl)-3,6-diazabicyclo[3.1.1]heptane 4c was found to be the most alpha7alpha4beta2 selective term in receptor binding assays (alpha7alpha4beta2=1295). Moreover, compound 4d also had high affinity for the alpha4beta2 nAChR subtype (K(i)=1.2 nM) with considerably high selectivity (alpha7/alpha4beta2=23300). |
| PubMedSearch : Murineddu_2008_Bioorg.Med.Chem.Lett_18_6147 |
| PubMedID: 18938077 |
Murineddu G, Murruzzu C, Curzu MM, Chelucci G, Gotti C, Gaimarri A, Legnani L, Toma L, Pinna GA (2008)
Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors
Bioorganic & Medicinal Chemistry Lett
18 :6147
Murineddu G, Murruzzu C, Curzu MM, Chelucci G, Gotti C, Gaimarri A, Legnani L, Toma L, Pinna GA (2008)
Bioorganic & Medicinal Chemistry Lett
18 :6147