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Dispirooxindole-β-Lactams: Synthesis via Staudinger Ketene-Imine Cycloaddition and Biological Evaluation

Title: Dispirooxindole-β-Lactams: Synthesis via Staudinger Ketene-Imine Cycloaddition and Biological Evaluation
Authors: Vadim E. Filatov; Dmitrii A. Iuzabchuk; Viktor A. Tafeenko; Yuri K. Grishin; Vitaly A. Roznyatovsky; Dmitrii A. Lukianov; Yulia A. Fedotova; Maxim A. Sukonnikov; Dmitry A. Skvortsov; Nikolai V. Zyk; Elena K. Beloglazkina
Source: International Journal of Molecular Sciences, Vol 23, Iss 6666, p 6666 (2022)
Publisher Information: MDPI AG
Publication Year: 2022
Collection: Directory of Open Access Journals: DOAJ Articles
Subject Terms: spirooxindoles; β-lactams; Staudinger reaction; ketene-imine cycloaddition; oxo-pyrrolidine-3-carboxylic acids; Biology (General); QH301-705.5; Chemistry; QD1-999
Description: In this work, we present the first synthesis of dispirooxindole-β-lactams employing optimized methodology of one-pot Staudinger ketene-imine cycloaddition with N-aryl-2-oxo-pyrrolidine-3-carboxylic acids as the ketene source. Spiroconjugation of indoline-2-one with β-lactams ring is considered to be able to provide stabilization and wide scope of functionalization to resulting scaffolds. The dispipooxindoles obtained demonstrated medium cytotoxicity in the MTT test on A549, MCF7, HEK293, and VA13 cell lines, and one of the compounds demonstrated antibacterial activity against E. coli strain LPTD.
Document Type: article in journal/newspaper
Language: English
Relation: https://www.mdpi.com/1422-0067/23/12/6666; https://doaj.org/toc/1661-6596; https://doaj.org/toc/1422-0067; https://doaj.org/article/4edefa4d04ee4dc6b4bffba83d29dc62
DOI: 10.3390/ijms23126666
Availability: https://doi.org/10.3390/ijms23126666; https://doaj.org/article/4edefa4d04ee4dc6b4bffba83d29dc62
Accession Number: edsbas.8CF1740
Database: BASE