1020153-63-2Relevant academic research and scientific papers
Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain
Díaz, José Luis,Cuevas, Félix,Oliva, Ana I.,Font, Daniel,Sarmentero, M. ángeles,álvarez-Bercedo, Paula,López-Valbuena, José M.,Pericàs, Miquel A.,Enrech, Raquel,Montero, Ana,Yeste, Sandra,Vidal-Torres, Alba,álvarez, Inés,Pérez, Pilar,Cendán, Cruz Miguel,Cobos, Enrique J.,Vela, José Miguel,Almansa, Carmen
, p. 5157 - 5170 (2021/05/07)
The synthesis and pharmacological activity of a new series of 5a,7,8,8a-tetrahydro-4H,6H-pyrrolo[3,4-b][1,2,3]triazolo[1,5-d][1,4]oxazine derivatives as potent sigma-1 receptor (σ1R) ligands are reported. A lead optimization program aimed at improving the aqueous solubility of parent racemic nonpolar derivatives led to the identification of several σ1R antagonists with a good absorption, distribution, metabolism, and excretion in vitro profile, no off-target affinities, and characterized by a low basic pKa (around 5) that correlates with high exposure levels in rodents. Two compounds displaying a differential brain-to-plasma ratio distribution profile, 12lR and 12qS, exhibited a good analgesic profile and were selected as preclinical candidates for the treatment of pain.
Synthesis and antiviral activity of novel spirocyclic nucleosides
Cobb, Alexander J. A.,Dell'Isola, Antonio,Abdulsattar, Ban O.,McLachlan, Matthew M. W.,Neuman, Benjamin W.,Müller, Christin,Shankland, Kenneth,Al-Mulla, Hawaa M. N.,Binks, Alexander W. D.,Elvidge, Warren
, p. 18363 - 18380 (2018/11/23)
The synthesis of a number of spirocyclic ribonucleosides containing either a triazolic or azetidinic system is described, along with two analogous phosphonate derivatives of the former. These systems were constructed from the same β-d-psicofuranose starti
Synthesis of Carbolines via Palladium/Carboxylic Acid Joint Catalysis
Cera, Gianpiero,Lanzi, Matteo,Balestri, Davide,Della Ca, Nicola,Maggi, Raimondo,Bigi, Franca,Malacria, Max,Maestri, Giovanni
supporting information, p. 3220 - 3224 (2018/06/11)
The combination of a Pd(0) complex with benzoic acid converts propargylic tryptamines to the corresponding tetrahydro-β-carbolines. The method uses unprotected indoles and affords the desired products with ample functional group tolerance. Detailed modeling studies reveal a close synergy between the organic and metal catalysts, which enables sequential alkyne isomerization, indole C-H activation, and eventual C-C reductive elimination to afford the target heterocycles.
Synthesis and antiviral properties of spirocyclic [1,2,3]-Triazolooxazine nucleosides
Dell'Isola, Antonio,McLachlan, Matthew M. W.,Neuman, Benjamin W.,Al-Mullah, Hawaa M. N.,Binks, Alexander W. D.,Elvidge, Warren,Shankland, Kenneth,Cobb, Alexander J. A.
supporting information, p. 11685 - 11689 (2014/10/15)
An efficient synthesis of spirocyclic triazolooxazine nucleosides is described. This was achieved by the conversion of β-D-psicofuranose to the corresponding azido-derivative, followed by alkylation of the primary alcohol with a range of propargyl bromide
Tricyclic triazolic compounds
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Page/Page column 20, (2009/07/10)
The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of
Intramolecular azide-Alkyne for the fast assembly of structurally diverse, tricyclic 1,2,3-triazoles
Oliva, Ana I.,Christmann, Ute,Font, Daniel,Cuevas, Flix,Ballester, Pablo,Buschmann, Helmut,Torrens, Antoni,Yenes, Susana,Perics, Miquel A.
supporting information; experimental part, p. 1617 - 1619 (2009/04/07)
The synthesis of novel tricyclic 1,2,3-triazoles starting from cyclic epoxides via the sequential azidolysis, propargylation and 1,3-dipolar cycloaddition is described. Derivatization by N-arylation reaction and the synthesis of enantiomerically pure comp
