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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.

Magdalena ŁysakowskaIwona E GłowackaGraciela AndreiDominique ScholsRobert SnoeckPaweł LisieckiMagdalena SzemrajDorota G Piotrowska
Published in: Molecules (Basel, Switzerland) (2022)
Dipolar cycloaddition of the N-substituted C -(diethoxyphosphonyl)nitrones with N 3 -allyl- N 1 -benzylquinazoline-2,4-diones produced mixtures of diastereoisomeric 3-(diethoxyphosphonyl)isoxazolidines with a N 1 -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 EC 50 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.
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