Biological Effects on μ-Receptors Affinity and Selectivity of Arylpropenyl Chain Structural Modification on Diazatricyclodecane Derivatives

Autor: Sandra Piras, Gabriele Murineddu, Giovanni Loriga, Antonio Carta, Enrica Battistello, Stefania Merighi, Stefania Gessi, Paola Corona, Battistina Asproni, Roberta Ibba, Veronika Temml, Daniela Schuster, Gérard Aimè Pinna

Publikováno v: Molecules, Vol 26, Iss 18, p 5448 (2021)

Opioid analgesics are clinically used to relieve severe pain in acute postoperative and cancer pain, and also in the long term in chronic pain. The analgesic action is mediated by μ-, δ-, and κ-receptors, but currently, with few exceptions for k-a

Externí odkaz: https://doaj.org/article/939248af90d64ab2817aedfd3ac68830

Development of Oxygen-Bridged Pyrazole-Based Structures as Cannabinoid Receptor 1 Ligands

Autor: Gabriele Murineddu, Battistina Asproni, Paola Corona, Sandra Piras, Paolo Lazzari, Stefania Ruiu, Laura Legnani, Lucio Toma, Gérard A. Pinna

Publikováno v: Molecules, Vol 24, Iss 9, p 1656 (2019)

In this work, the synthesis of the cannabinoid receptor 1 neutral antagonists 8-chloro-1-(2,4-dichlorophenyl)-N-piperidin-1-yl-4,5-dihydrobenzo-1H-6-oxa-cyclohepta[1,2-c]pyrazole-3-carboxamide 1a and its deaza N-cyclohexyl analogue 1b has led to a de

Externí odkaz: https://doaj.org/article/876b14a9242348abb1c31316f7cef201

Synthesis and Cytotoxicity of Novel Hexahydrothienocycloheptapyridazinone Derivatives

Autor: Irene Marchesi, Maria M. Curzu, Gérard A. Pinna, Giuseppe E. Grella, Caterina Murruzzu, Battistina Asproni, Amedeo Pau, Gabriele Murineddu, Luigi Bagella

Publikováno v: Molecules, Vol 14, Iss 9, Pp 3494-3508 (2009)

Designed as a new group of tricyclic molecules containing the thienocycloheptapyridazinone ring system, a number of 2N-substituted-hexahydrothienocycloheptapyridazinone derivatives were synthesized and their biological activity evaluated. Among the s

Externí odkaz: https://doaj.org/article/a90cefac57774239ba6e4f35ec862bc1

Novel 1,3,4-oxadiazole chalcogen analogues: Synthesis and cytotoxic activity

Autor: Stefano, Zoroddu, Paola, Corona, Luca, Sanna, Federica, Borghi, Valentina, Bordoni, Battistina, Asproni, Gerard A, Pinna, Luigi, Bagella, Gabriele, Murineddu

Publikováno v: European Journal of Medicinal Chemistry. 238:114440

A small library of novel 1,3,4-oxadiazole bioisosteres was synthesized and their cytotoxic activity evaluated in vitro. Five of the new derivatives (3, 6, 11, 14 and 15) showed high potency against different human cancer cell lines, with 14 being the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a4fcaba53578fbf459f6dc475b399d2
https://doi.org/10.1016/j.ejmech.2022.114440

Pyridinyl- and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for α4β2 nACh receptors

Autor: Cecilia Gotti, Gérard Aimé Pinna, Miriam Sciaccaluga, Gabriele Murineddu, Francesca Fasoli, Giovanni Loriga, Simona Plutino, Sergio Fucile, Francesco Deligia, Giulio Ragusa, Battistina Asproni

Publikováno v: European journal of medicinal chemistry 152 (2018): 401–416. doi:10.1016/j.ejmech.2018.04.026
info:cnr-pdr/source/autori:Deligia, F.; Murineddu, G.; Gotti, C.; Ragusa, G.; Fasoli, F.; Sciaccaluga, M.; Plutino, S.; Fucile, S.; Loriga, G.; Asproni, B.; Pinna, G. A./titolo:Pyridinyl-and pyridazinyl-3,6-diazabicyclo[3.1.1]heptane-anilines: Novel selective ligands with subnanomolar affinity for ?4<%2Finf>?2<%2Finf>nACh receptors/doi:10.1016%2Fj.ejmech.2018.04.026/rivista:European journal of medicinal chemistry/anno:2018/pagina_da:401/pagina_a:416/intervallo_pagine:401–416/volume:152

The cholinergic pathways in the central nervous system (CNS) of animals and humans are important for cognitive and behavioural functions. Until a few years ago, it was thought that the key molecules transducing the cholinergic message were the metabo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0da655537ee6484da71bef676693dd02
https://doi.org/10.1016/j.ejmech.2018.04.026