Results 71 to 80 of about 24,184 (203)

Von In‐Silico bis In‐Cerebro – Entwicklung des Orexinrezeptor Antagonisten „Photorexant“ zur Photomodulation In Vitro und im Gehirn der Maus

Angewandte Chemie, EarlyView.
Durch einen strukturbasierten Designansatz wurden photoschaltbare Derivate des von der FDA zugelassenen Arzneistoffes Suvorexant entwickelt, gedockt, synthetisiert und pharmakologisch an den Orexin‐1‐ und 2‐Rezeptoren (OX1R und OX2R) charakterisiert.
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

On the Evolvability of OXA-48. A comprehensive study of new functions within the β-lactamase OXA-48

, 2021
Our understanding of how antimicrobial resistance enzymes evolve to expand their substrate spectrum is limited. OXA-48, an enzyme able to catalyse the hydrolysis of β-lactam drugs, has become one of the most successfully disseminating β-lactamases. Although OXA-48 hydrolyses penicillins with high efficiency, its activity towards oxyimino cephalosporins,
openaire   +1 more source

Carbapenem Resistance of OXA-48 Gene Coding in Klebsiella Pneumoniae and Escherichia Coli

Annals of Mechnikov's Institute, 2021
Introduction: Bacteria that treated with antibiotics has ability to adapt or mutate due to form a defend mechanism. OXA-48 produces isolate that have ability as a resistance to drugs and all β-lactam, including cephalosporin, cephamycin, monobactone, and
Nita Parisa, Muhammad Fitrizal, Ella Amalia   +2 more
doaj  

In Silico to In Cerebro—Development of the Orexin Receptor Antagonist “Photorexant” for Photomodulation In Vitro and in Mouse Brains

Angewandte Chemie International Edition, EarlyView.
Following a structure‐based design approach, photoswitchable derivatives of the FDA‐approved drug suvorexant were designed, docked, synthesized, and characterized pharmacologically at the orexin 1 and 2 receptors (OX1R and OX2R). Optimized “photorexant” showed up to an 11‐fold difference in IC50 between photoisomers, enabled dynamic and reversible ...
Marcus Angermann, Marie H. Deventer, Vicente Ledesma‐Martin, Nuno Martinho, Alix Flake, Silvia Mori, Angel Nuñez, Jaime Pignatelli, Rita C. Guedes, Christophe P. Stove, Michael Decker   +10 more
wiley   +1 more source

The One‐Step Synthesis of Biologically Active Isochromans from Lignin‐Derived Aromatic Monomers in Tunable Deep Eutectic Solvents

Chemistry – A European Journal, EarlyView.
A straightforward one‐step protocol enables the synthesis of bio‐based and biologically active isochromans through the Oxa‐Pictet cyclization involving diverse aldehydes, including vanillin in combination with lignin‐derivable homovanillyl alcohol, a prominent aromatic platform chemical obtainable via diol‐assisted fractionation of lignocellulose ...
Anjali Kottayi, Anastasiia M. Afanasenko, Antonio A. Castillo‐Garcia, Walid A. M. Elgaher, Jörg Haupenthal, Anna K. H. Hirsch, Katalin Barta   +6 more
wiley   +1 more source

Detection of OXA-181/OXA-48 carbapenemase producing Enterobacteriaceae in Bangladesh

IMC Journal of Medical Science, 2015
Carbapenem resistant Enterobacteriaceae (CRE) is becoming a major public health concern globally. Detection of carbapenem hydrolyzing enzyme carbapenemase in Enterobacteriaceae is important to institute appropriate therapy and to initiate preventive ...
Rehana Khatun, S.M. Shamsuzzaman
doaj  

Photochemistry of Aromatic N‐Oxides in Water Probed by Time‐Resolved X‐ray Absorption Spectroscopy

Chemistry – A European Journal, EarlyView.
Time‐resolved XAS at the nitrogen and oxygen K‐edges is applied to the photorearrangement of two N‐oxides in water. Pyridine N‐oxide rapidly forms the oxaziridine isomer. Pyridazine N‐oxide undergoes ring opening to the diazo compound, without any evidence of intermediates.
Maximilian Paradiz Domínguez, Robby Büchner, Mattis Fondell, Albert M. Brouwer   +3 more
wiley   +1 more source

Strain Release of 1‐Azabicyclo[1.1.0]butanes as a Gateway to Highly Functionalized Azetidines: New Strategies and Structural Motifs

Chemistry – A European Journal, EarlyView.
Over the past decade, the interest in azetidines has continuously risen, by virtue of their highly appealing pharmaceutical properties. Monocyclic, spirocyclic, and bridged azetidines can be accessed by leveraging 1‐azabicyclo[1.1.0]butanes as precursors.
Yuri Gelato, Philipp Natho, Marco Colella, Renzo Luisi   +3 more
wiley   +1 more source

WGS-based characterization of trans-sectoral OXA-48-producing Escherichia coli in Switzerland

One Health Advances
The broad trans-sectoral (humans, animals, environment) dissemination potential of OXA-48 carbapenemase-producing Escherichia coli (OXA-48-Ec) and OXA-48-harboring plasmids represent a major One-Health concern.
Valentina Donà, Patrice Nordmann, Javier E. Fernandez, Laurent Poirel, Jacqueline Findlay, Simone Schuller, Sonja Kittl, Helene Rohrbach, Andrea Endimiani, Vincent Perreten   +9 more
doaj   +1 more source

Flipping the Card With Enantiodivergent Organocatalysis

Chemistry – A European Journal, EarlyView.
This minireview elaborates on recent organocatalytic strategies for achieving enantiodivergence—the ability to access both product enantiomers using a single chiral catalyst. It highlights how achiral stimuli, such as solvent polarity and chemical additives, along with minimal catalyst modifications, trigger stereochemical inversions in reactions ...
Debora Iapadre, Alessio Carioscia, Alessandro Brusa, Armando Carlone   +3 more
wiley   +1 more source