Design, synthesis, and antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton

Herein we report a feasible study concerning the design, synthesis, and in vitro antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton. The reaction pathway is efficient and straight, involving the direct N-acylation of diazine with homodrimane sesquiterpenoids bear...

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Veröffentlicht in:Medicinal chemistry research 2014-03, Vol.23 (3), p.1559-1568
Hauptverfasser: Kuchkova, Kaleria, Aricu, Aculina, Secara, Elena, Barba, Alic, Vlad, Pavel, Ungur, Nicon, Tuchilus, Cristina, Shova, Sergiu, Zbancioc, Gheorghita, Mangalagiu, Ionel I.
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Sprache:eng
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Zusammenfassung:Herein we report a feasible study concerning the design, synthesis, and in vitro antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton. The reaction pathway is efficient and straight, involving the direct N-acylation of diazine with homodrimane sesquiterpenoids bearing acyl chlorides or organic acids functionality. A reliable explication and a feasible reaction mechanism for the obtained compounds are presented. The in vitro antimicrobial activity of the homodrimane sesquiterpenoids with and without diazine skeleton has been evaluated. All the tested compounds have an excellent antibacterial activity against Gram-positive strains S. aureus and B. cereus . SAR correlations concerning antimicrobial activity are reported. Graphical Abstract The design, synthesis, and in vitro antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton are described. Antimicrobial tests prove that some homodrimane sesquiterpenoids have an excellent biological activity.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-013-0720-3