106880-69-7Relevant academic research and scientific papers
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 (2020)
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.
Contrast enhancement agents and method of use thereof
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Page/Page column 57-58, (2015/11/09)
A contrast agent composition and a method of diagnostic imaging are provided. The composition comprises a pharmaceutically acceptable carrier and a metal-complex comprising a ligand having structure (XXX): wherein R1, R2, R3/su
(1, 10B-DIHYDRO-2-(AMINOALKYL- PHENYL)-5H-PYRAZ0L0 [1,5-C] [1,3] BENZ0XAZIN-5-YL) PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLIATION INHIBITORS
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Page/Page column 28, (2008/06/13)
The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, a
(1,10B-DIHYDRO-2-(AMINOCARBONYL-PHENYL)-5H-PYRAZOLO[1,5- C][1,3]BENZOXAZIN-5-YL)PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLICATION INHIBITORS
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Page/Page column 26, (2010/02/14)
The present invention relates to 5H-pyrazolo[1,5-c] [1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines,
BREAST CANCER RESISTANCE PROTEIN (BCRP) INHIBITOR
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Page/Page column 14, (2010/02/14)
The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (-NHCOCH3 group), a cyano group (-CN group), a formyl group (-CHO group), -COOR1 (R1 is hydrogen or C1-C4 alkyl) , -O(CH2)nCOOR2 (n=1-7: R2 is hydrogen or C1-C4 alkyl) , -OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., -OP(O) (OH)2) or a salt thereof, a sulfate group (i.e., -OSO3H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
Hydrolysis of an Amide in a Carboxypeptidase Model Using Co(III) and Bifunctional Catalysts
Schepartz, Alanna,Breslow, Ronald
, p. 1814 - 1826 (2007/10/02)
The ability of a metal ion to cooperate with various inter- and intramolecular acids and bases and promote amide hydrolysis has been investigated.Phenolic and carboxylic functional groups were placed within reach of Co(III)-chelated amides in complexes th
