6109-54-2Relevant articles and documents
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype
Bavo, Francesco,Pallavicini, Marco,Gotti, Cecilia,Appiani, Rebecca,Moretti, Milena,Colombo, Sara Francesca,Pucci, Susanna,Viani, Paola,Budriesi, Roberta,Renzi, Massimiliano,Fucile, Sergio,Bolchi, Cristiano
, p. 15668 - 15692 (2021/01/09)
A series of diastereomeric 2-(2-pyrrolidinyl)-1,4-benzodioxanes bearing a small, hydrogen-bonding substituent at the 7-, 6-, or 5-position of benzodioxane have been studied for α4β2 and α3β4 nicotinic acetylcholine receptor affinity and activity. Analogous to C(5)H replacement with N and to a much greater extent than decoration at C(7), substitution at benzodioxane C(5) confers very high α4β2/α3β4 selectivity to the α4β2 partial agonism. Docking into the two receptor structures recently determined by cryo-electron microscopy and site-directed mutagenesis at the minus β2 side converge in indicating that the limited accommodation capacity of the β2 pocket, compared to that of the β4 pocket, makes substitution at C(5) rather than at more projecting C(7) position determinant for this pursued subtype selectivity.
6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA
Tanc, Muhammet,Carta, Fabrizio,Scozzafava, Andrea,Supuran, Claudiu T.
supporting information, p. 77 - 80 (2015/01/09)
A series of 6-substituted 2-benzoxathiine-2,2-dioxides were synthesized starting from 2,5-dihydroxybenzaldehyde, and then screened in vitro for their inhibition properties against five human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms. All the compounds
SAR studies of epoxycurcuphenol derivatives on leukemia CT-CD4 cells
Galindo, José L.G.,Macías, Mariola,Molinillo, José M.G.,Mu?oz-Suano, Alba,Torres, Ascensión,Varela, Rosa M.,García-Cozar, Francisco,Macías, Francisco A.
supporting information, p. 6662 - 6668 (2013/01/15)
Bioactive natural products are a potential source of new pharmaceuticals since they offer new modes of action and more specific activities. The use of derivatization also enables the optimal structure for their biological activity to be determined. In thi