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VNI cures acute and chronic experimental Chagas disease.
TLDR
VNI is a potent experimental inhibitor of T. cruzi sterol 14α-demethylase that displays promising pharmacokinetics and administered orally to mice at 25 mg/kg for 30 days cures, with 100% cure rate and 100% survival, the acute and chronic T.cruzi infection. Expand
Catalytic, Enantioselective Synthesis of Stilbene cis-Diamines: A Concise Preparation of (-)-Nutlin-3, a Potent p53/MDM2 Inhibitor.
TLDR
The first highly diastereo- and enantioselective additions of aryl nitromethane pronucleophiles to aryL aldimines are described, leading ultimately to differentially protected cis-stilbene diamines in two steps. Expand
Preparation of a protected phosphoramidon precursor via an H-phosphonate coupling strategy.
TLDR
The preparation of a phosphoramidon precursor is described using a phosphorus(III) coupling protocol and its application in selective separation of Na6(II) from Na3SO4 and Na2SO4 is described. Expand
A convergent synthesis of 1,3,4-oxadiazoles from acyl hydrazides under semiaqueous conditions† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c7sc00195a Click here for
An innovative new synthesis approach to disubstituted 1,3,4-oxadiazoles is described, inspired by Umpolung Amide Synthesis (UmAS).
Development of an Intermittent-Flow Enantioselective Aza-Henry Reaction Using an Arylnitromethane and Homogeneous Brønsted Acid-Base Catalyst with Recycle.
TLDR
This work demonstrates the advantages of a novel intermittent-flow setup with product crystallization and slow reagent addition which is not amenable to the standard continuous equipment: plug flow tube reactor (PFR) or continuous stirred tank reactor (CSTR). Expand
MDM2 Antagonists Counteract Drug-Induced DNA Damage
TLDR
It is discovered that MDM2-p53 antagonists protect DNA from drug-induced damage in melanoma cells and patient-derived xenografts and targeting p21 can improve the efficacy of such combinations of anti-cancer drugs. Expand
A case study in biomimetic total synthesis: polyolefin carbocyclizations to terpenes and steroids.
TLDR
I would like to give a warning, from a theoretical point of view, about all the carbonium ion mechanisms, that the human mind is not quick and clever as the enzyme. Expand
‘Umpolung’ Reactivity in Semiaqueous Amide and Peptide Synthesis
TLDR
The use of nitroalkanes as acyl anion equivalents provides a conceptually innovative approach to amide and peptide synthesis, and one that might ultimately provide for efficient peptides and proteins synthesis that is fully reliant on enantioselective methods. Expand
Chiral proton catalysis: a catalytic enantioselective direct aza-Henry reaction.
TLDR
This discovery suggests the use of ionic hydrogen bonds in asymmetric catalysis may not only be more general than previously thought, but also a viable "green" approach to single-enantiomer organic compounds. Expand
Achiral counterion control of enantioselectivity in a Brønsted acid-catalyzed iodolactonization.
TLDR
An approach that modulates the achiral counterion (equimolar to the neutral chiral ligand-proton complex present at low catalyst loadings) to optimize the enantioselection is documented for the first time in this transformation. Expand
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