Stille vs. Suzuki – cross-coupling for the functionalization of diazocines

RSC Advances, Год журнала: 2023, Номер 13(23), С. 15805 - 15809

Опубликована: Янв. 1, 2023

Efficient syntheses towards stannylated and borylated diazocines are presented which subsequently employed in Stille Suzuki cross-coupling reactions.

Язык: Английский

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A functionalized CNT-azobenzene-PVA-based self-healing aqueous gel as a conductive photo-responsive actuator

Journal of Materials Chemistry C, Год журнала: 2023, Номер 11(47), С. 16571 - 16577

Опубликована: Янв. 1, 2023

Responsive conductive gels have gained attention owing to potential applications in flexible displays, implantable medical devices, touch panels, wearable electronic skin, sensors, soft robotics, and related areas .

Язык: Английский

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Light-controlled inhibition of the circadian regulator RORγ

Опубликована: Июль 31, 2023

Retinoic acid receptor-related orphan receptor γ (RORγ) is a circadian regulator and has emerged as experimental therapeutic target in inflammation immunity. The cyclic temporal role of RORγ rhythms makes temporally-resolved pharmacological control this particularly intriguing. To achieve next-generation tools to study biology, we designed ligands featuring central azobenzene photoswitch, that act light-dependent inverse agonists. Structural optimization enabled efficient photocontrol over inhibition, with remarkable potency on excellent selectivity related receptors. These high-specificity photopharmaceuticals can serve high-precision the dynamic modulation signaling pathways inflammatory disorders.

Язык: Английский

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Synthesis and crystal structure of tetramethyl (E)-4,4′-(ethene-1,2-diyl)bis(5-nitrobenzene-1,2-dicarboxylate)

Acta Crystallographica Section E Crystallographic Communications, Год журнала: 2024, Номер 80(4), С. 435 - 438

Опубликована: Март 28, 2024

The title compound, C 22 H 18 N 2 O 12 , was obtained as a by-product during the planned synthesis of 1,2-bis(2-nitro-4,5-dimethyl phthalate)ethane by oxidative dimerization starting from dimethyl-4-methyl-5-nitro phthalate. To identify this compound unambiguously, single-crystal structure analysis performed. asymmetric unit consists half molecule that is located at centre inversion. As result symmetry restrictions, shows an E configuration around double bond. Both phenyl rings are coplanar, whereas nitro and two methyl ester groups rotated out ring plane 32.6 (1), 56.5 (2) 49.5 (2)°, respectively. In crystal, molecules connected into chains extending parallel to axis pairs C—H...O hydrogen bonds tri-periodic network additional hydrogen-bonding interactions.

Язык: Английский

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A High‐Quality Photoswitchable Probe that Selectively and Potently Regulates the Transcription Factor RORγ

Angewandte Chemie, Год журнала: 2024, Номер 136(49)

Опубликована: Сен. 9, 2024

Abstract Der Retinsäure‐Rezeptor‐verwandte Waisen‐Rezeptor γ (RORγ) ist ein nuklearer Hormonrezeptor mit vielfältigen biologischen Funktionen in der Regulation zirkadianen Uhr, bei Entzündungen und Immunität. Seine zyklisch‐zeitliche Rolle Rhythmen seine zellspezifische Aktivität im Immunsystem machen ihn zu einer interessanten Zielstruktur für die räumlich zeitlich lokalisierte Pharmakologie. Um Werkzeuge entwickeln, denen RORγ‐Biologie angemessener räumlicher zeitlicher Auflösung untersucht werden kann, haben wir durch Einbau von Azobenzol‐Photoschaltern Liganden‐Konsensstrukturen lichtabhängige inverse RORγ‐Agonisten entwickelt. Strukturoptimierungen führten photoschaltbaren RORγ‐Inhibitoren, hohes Maß an Licht‐kontrollierter bemerkenswerter On‐Target‐Potenz hervorragender Selektivität gegenüber verwandten Rezeptoren kombinieren. Diese auf dem Gebiet Photopharmakologie seltene Qualität zeichnet sie als hochwertige photoschaltbare Sonden aus, nun hochpräzise zur Untersuchung räumlichen dynamischen Feinheiten RORγ‐Wirkung Signalübertragung entzündlichen Erkrankungen dienen können.

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