Wir präsentieren eine Nanodroplet‐Array‐Plattform, die die Integration von Festphasensynthese, MALDI‐MS‐Analyse und zellbasiertem Screening von 325 potenziellen MEK‐Inhibitoren (Mitogen‐aktivierte‐Proteinkinase‐Kinase) in Nanoliter‐Volumina ermöglicht.
Maximilian Seifermann +10 more
wiley +1 more source
N-Butylpyrrolidinone as a dipolar aprotic solvent for organic synthesis [PDF]
Dipolar aprotic solvents such as N-methylpyrrolidinone (or 1-methyl-2-pyrrolidone (NMP)) are under increasing pressure from environmental regulation. NMP is a known reproductive toxin and has been placed on the EU “Substances of Very High Concern” list ...
Farmer, Thomas James +4 more
core +1 more source
Regulierung der Promiskuitiven Katalyse durch Substratinduzierte Transiente Assemblierung
Wir berichten über eine neuartige substratinduzierte transiente Koassemblierung zwischen einem kurzen lysinreichen Peptid und Fmoc‐Gly‐OH. Im aktivierten Zustand zeigt die Assemblierung eine promiskuitive katalytische Aktivität durch die Beschleunigung der Hydrolyse und der C═N‐Kondensationsreaktion.
Ayan Chatterjee +7 more
wiley +1 more source
Opportunities and challenges for direct C–H functionalization of piperazines
Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C–H functionalization on piperazines in order to lend ...
Zhishi Ye, Kristen E. Gettys, Mingji Dai
doaj +1 more source
1,3-Dipolar cycloadditions of 2-thio-3-chloroacrylamides with nitrile oxides and nitrones [PDF]
1,3-Dipolar cycloadditions of 2-thio-3-chloroacrylamides with nitrile oxides and nitrones is described. A series of novel isoxazolines are isolated from the nitrile oxide cycloadditions, whilst the isoxazolines generated from the nitrone cycloadditions ...
Kissane, Marie +2 more
core +1 more source
Diastereoselective synthesis of some novel benzopyranopyridine derivatives
BackgroundThe formation of novel N-substituted-1,2,3,4-tetrahydro[1,3]-dioxolo-[6,7]-5H-[1]benzopyrano [3,4-c]pyridines were observed unexpectedly during the acid-mediated ketal removal of ethylenedioxy ketal protected 4-piperidones.
Pradeep K. Mohakhud +6 more
doaj +1 more source
Plant enzyme reactions leading to the formation of heterocyclic compounds. 1. The formation of unsaturated pyrrolidine and piperidine compounds [PDF]
P. J. Mann, W. R. Smithies
openalex +1 more source
The Synthesis and Biological Activity of 1-Alkyl-4-(3-azacyclobenzoyl)-5-hydroxypyrazole Herbicides
The benzoylpyrazoles belong to a class of herbicides that inhibit the enzyme 4-hydroxy-phenylpyruvate dioxygenase (HPPD). This mode of action is characterized by bleaching due to the disruption of plastoquinone and ?-tocopherol biosynthesis ...
Zoltan Benko +8 more
doaj +1 more source
Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor [PDF]
L-glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) and plays a fundamental role in the control of motor function, cognition and mood.
Grove, Simon J .A. +4 more
core +1 more source
Diels-alder cycloaddition in the synthesis of 1-azafagomine, analogs, and derivatives as glycosidase inhibitors [PDF]
This comprehensive review deals with the synthesis of 1-azafagomine, analogs, and derivatives having the Diels-Alder cycloaddition as the key step. Most of the compounds referred are racemic or have been resolved by lipase transesterification.
Alves, M. José +3 more
core +1 more source

