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- Title
Design, Synthesis, Anti-Varicella-Zoster and Antimicrobial Activity of (Isoxazolidin-3-yl)Phosphonate Conjugates of N1-Functionalised Quinazoline-2,4-Diones.
- Authors
Łysakowska, Magdalena; Głowacka, Iwona E.; Andrei, Graciela; Schols, Dominique; Snoeck, Robert; Lisiecki, Paweł; Szemraj, Magdalena; Piotrowska, Dorota G.
- 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.
- Subjects
ISOXAZOLIDINES; ANTI-infective agents; ANTIBACTERIAL agents; NITRONES; MUTAGENS; RING formation (Chemistry)
- Publication
Molecules, 2022, Vol 27, Issue 19, p6526
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules27196526