5,6-Dihydro-2H-pyran-3(4H)-on als Baustein zur Synthese pyrananellierter Heterocyclen [PDF]
, 1984 Während 5,6-Dihydro-2H-pyran-3(4H)-on (3) sich mit ortho-substituierten Phenylcarbonylverbindungen nur in Einzelfällen regioselektiv zu pyrananellierten Heterocyclen umsetzt - z. B.
Eiden, Fritz, Wanner, Klaus Th.
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Benzothiazole durch C-C-Spaltung von alpha-[(2-Nitrophenyl)thio]ketonen [PDF]
, 1984 Einwirkung von Ammoniak bzw. Natronlauge auf die -[(2-Nitrophenyl)thio]ketone 4, 11a-c und 16 führt unter CC-Spaltung zu den Benzothiazol-N-oxid-Derivaten 8, 12ac und 17; aus dem 3-[(2-Nitrophenyl)thio]-4-piperidon-Derivat 22 entsteht der 2 ...
Babichev +10 more
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Positive allosteric modulators of the a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor [PDF]
, 2010 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
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Intramolecular Azide to Alkene Cycloadditions for the Construction of Pyrrolobenzodiazepines and Azetidino-Benzodiazepines [PDF]
, 2014 The coupling of proline- and azetidinone-substituted alkenes to 2-azidobenzoic and 2-azidobenzenesulfonic acid gives precursors that undergo intramolecular azide to alkene 1,3-dipolar cycloadditions to give imine-, triazoline- or aziridine-containing ...
Antonow +9 more
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Chiral benzimidazoles as hydrogen bonding organocatalysts [PDF]
, 2015 Several bifunctional organocatalysts bearing the benzimidazole unit have been designed in order to act as bifunctional systems by hydrogen bonding. Chiral 2-aminobenzimidazoles are conformational rigid guanidines able to catalyze enantioselectively ...
Nájera, Carmen, Yus, Miguel
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Electrically Driven N(sp 2)- C(sp 2/3) Bond Cleavage of Sulfonamides [PDF]
, 2020 Sulfonamides are a privileged class of functional groups in medicinal chemistry and an important class of protecting groups in organic synthesis. We report the discovery and development of unexpected electrically driven N(sp2)-C(sp2) and N(sp2)-C(sp3 ...
Jones, Alan M., Wetzel, Annica
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A case of insulinoma effectively treated with low‐dose diazoxide
Clinical Case Reports, Volume 8, Issue 10, Page 1884-1889, October 2020., 2020 Diazoxide is a benzothiadiazine that can be effective in managing hypoglycemia in frail patients with surgical risk. We report here a case of insulinoma effectively treated with diazoxide, as our report will be helpful for similar cases. Abstract Diazoxide is a benzothiadiazine that can be effective in managing hypoglycemia in frail patients with ...
Atsushi Yasuda +8 more
wiley +1 more source
A multivariate analysis on non-nucleoside HIV-1 reverse transcriptase inhibitors and resistance induced by mutation [PDF]
, 2004 This paper describes the use of multivariate statistical procedure PCA as a tool to explore the inhibitory activity of classes of NNRTIs against HIV-1 viruses (wild type and more frequent mutants, Y181C, V106A, K103N, L100I) and against RT enzyme.
Arranz +16 more
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Pharmmaker: Pharmacophore modeling and hit identification based on druggability simulations
Protein Science, Volume 29, Issue 1, Page 76-86, January 2020., 2020 Abstract Recent years have seen progress in druggability simulations, that is, molecular dynamics simulations of target proteins in solutions containing drug‐like probe molecules to characterize their drug‐binding abilities, if any. An important consecutive step is to analyze the trajectories to construct pharmacophore models (PMs) to use for virtual ...
Ji Young Lee +3 more
wiley +1 more source
Heterocycle-based bifunctional organocatalysts in asymmetric synthesis [PDF]
, 2016 Different chiral bifunctional organocatalysts derived from trans-cyclohexane-1,2-diamine bearing different types of guanidine units able to form-hydrogen bonding activation have been designed. Conformational rigid 2-aminobenzimidazoles bearing a tertiary
Gómez Bengoa, Enrique +2 more
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