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1.
Bioorg Med Chem ; 100: 117618, 2024 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-38309201

RESUMEN

The virally encoded 3C-like protease (3CLpro) is a well-validated drug target for the inhibition of coronaviruses including Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). Most inhibitors of 3CLpro are peptidomimetic, with a γ-lactam in place of Gln at the P1 position of the pseudopeptide chain. An effort was pursued to identify a viable alternative to the γ-lactam P1 mimetic which would improve physicochemical properties while retaining affinity for the target. Discovery of a 2-tetrahydrofuran as a suitable P1 replacement that is a potent enzymatic inhibitor of 3CLpro in SARS-CoV-2 virus is described herein.


Asunto(s)
Antivirales , Inhibidores de Proteasa de Coronavirus , Furanos , Antivirales/química , Antivirales/farmacología , Lactamas , Péptido Hidrolasas , Inhibidores de Proteasas/farmacología , Inhibidores de Proteasas/química , SARS-CoV-2 , Furanos/química , Inhibidores de Proteasa de Coronavirus/química
2.
Org Lett ; 17(13): 3370-3, 2015 Jul 02.
Artículo en Inglés | MEDLINE | ID: mdl-26099020

RESUMEN

The non-nucleophilic organic superbase P2Et phosphazene can enable a broad range of palladium-catalyzed cross-coupling reactions, including C-C, C-N, and C-O couplings of aryl chlorides, bromides, and iodides at room temperature. The mildness and substrate compatibility of this chemistry can deliver immediate synthetic utility for the preparation of complex molecules.

3.
Science ; 347(6217): 49-53, 2015 Jan 02.
Artículo en Inglés | MEDLINE | ID: mdl-25554781

RESUMEN

At the forefront of new synthetic endeavors, such as drug discovery or natural product synthesis, large quantities of material are rarely available and timelines are tight. A miniaturized automation platform enabling high-throughput experimentation for synthetic route scouting to identify conditions for preparative reaction scale-up would be a transformative advance. Because automated, miniaturized chemistry is difficult to carry out in the presence of solids or volatile organic solvents, most of the synthetic "toolkit" cannot be readily miniaturized. Using palladium-catalyzed cross-coupling reactions as a test case, we developed automation-friendly reactions to run in dimethyl sulfoxide at room temperature. This advance enabled us to couple the robotics used in biotechnology with emerging mass spectrometry-based high-throughput analysis techniques. More than 1500 chemistry experiments were carried out in less than a day, using as little as 0.02 milligrams of material per reaction.


Asunto(s)
Ensayos Analíticos de Alto Rendimiento/métodos , Nanopartículas , Nanotecnología/métodos , Preparaciones Farmacéuticas/síntesis química , Biotecnología , Catálisis , Espectrometría de Masas , Paladio/química , Robótica/métodos
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