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Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors

Murineddu, Gabriele and Murruzzu, Caterina and Curzu, Maria Michela and Chelucci, Giorgio Adolfo and Gotti, Cecilia and Gaimarri, Annalisa and Legnani, Laura and Toma, Lucio and Pinna, Gérard Aimé (2008) Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors. Bioorganic & Medicinal Chemistry Letters, Vol. 18 (23), p. 6147-6150. ISSN 0960-894X. Article.

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DOI: 10.1016/j.bmcl.2008.10.002


Α series of novel 3,6-diazabicyclo[3.1.1]heptane derivatives 4a–f was synthesized and their affinity and selectivity towards α4β2 and α7 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 α4β2 (Ki at α4β2 ranging from 0.023 to 0.056 nM) versus α7 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 α7α4β2 selective term in receptor binding assays (α7α4β2 = 1295). Moreover, compound 4d also had high affinity for the α4β2 nAChR subtype (Ki = 1.2 nM) with considerably high selectivity (α7/α4β2 = 23300).

Item Type:Article
ID Code:1387
Uncontrolled Keywords:3,6-Diazabicyclo[3.1.1]heptanes, neuronal nicotinic acetylcholine receptors, binding affinity, modeling
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Pergamon-Elsevier Science
Copyright Holders:© 2008 Elsevier Science
Additional Information:Pubblicato online il 5 ottobre 2008.
Deposited On:18 Aug 2009 10:05

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