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MDPI, Molecules, 19(27), p. 6526, 2022

DOI: 10.3390/molecules27196526

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Design, Synthesis, Anti-Varicella-Zoster and Antimicrobial Activity of (Isoxazolidin-3-yl)Phosphonate Conjugates of N1-Functionalised Quinazoline-2,4-Diones

Journal article published in 2022 by Magdalena Łysakowska ORCID, Iwona E. Głowacka ORCID, Graciela Andrei ORCID, Dominique Schols ORCID, Robert Snoeck, Paweł Lisiecki ORCID, Magdalena Szemraj ORCID, Dorota G. Piotrowska ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

Dipolar cycloaddition of the N-substituted C-(diethoxyphosphonyl)nitrones with N3-allyl-N1-benzylquinazoline-2,4-diones produced mixtures of diastereoisomeric 3-(diethoxyphosphonyl)isoxazolidines with a N1-benzylquinazoline-2,4-dione unit at C5. The obtained compounds were assessed for antiviral and antibacterial activities. Several compounds showed moderate inhibitory activities against VZV with EC50 values in the range of 12.63–58.48 µM. A mixture of isoxazolidines cis-20c/trans-20c (6:94) was found to be the most active against B. cereus PCM 1948, showing an MIC value 0.625 mg/mL, and also was not mutagenic up to this concentration.