117235-22-0Relevant articles and documents
ANTI-INFECTIVE HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Page/Page column 18; 68; 69, (2019/05/22)
The present invention relates to heterocyclic compounds of Formula F-I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.
New synthetic approach to paullones and characterization of their SIRT1 inhibitory activity
Soto, Sara,Vaz, Esther,Dell'Aversana, Carmela,Alvarez, Rosana,Altucci, Lucia,De Lera, Angel R.
supporting information; experimental part, p. 2101 - 2112 (2012/04/23)
A series of 7,12-dihydroindolo[3,2-d][1]benzazepine-6(5H)-ones (paullones) substituted at C9/C10 (Br) and C2 (Me, CF3, CO2Me) have been synthesized by a one-pot Suzuki-Miyaura cross-coupling of an o-aminoarylboronic acid and methyl 2-iodoindoleacetate followed by intramolecular amide formation. Other approaches to the paullone scaffold based on Pd-catalyzed C-H activation were unsuccessful. In vitro enzymatic assay with recombinant human SIRT-1 indicated a strong inhibitory profile for the series, in particular the analogue with a methoxycarbonyl group at C2 and a bromine at C9. These compounds are, in general, inducers of granulocyte differentiation of the U937 acute leukemia cell line and cause a marked increase in pre-G1 of the cell cycle.
Organocatalyzed enantioselective fluorocyclizations
Lozano, Oscar,Blessley, George,Martinez Del Campo, Teresa,Thompson, Amber L.,Giuffredi, Guy T.,Bettati, Michela,Walker, Matthew,Borman, Richard,Gouverneur, Veronique
supporting information; experimental part, p. 8105 - 8109 (2011/10/03)
Enantioenriched fluorinated heterocycles can be prepared through fluorocyclizations of prochiral indoles (see scheme; Ts=tosyl, Bn=benzyl, Boc=tert-butoxycarbonyl). More than twenty examples for this cascade fluorination-cyclization, which is catalyzed by cinchona alkaloids and employs N-fluorobenzenesulfonimide as the electrophilic fluorine source have been explored, and an unprecedented catalytic asymmetric difluorocyclization has also been identified.