Document Detail

Novel 1,2,5-oxadiazine derivatives--synthesis and in vitro biological studies.
MedLine Citation:
PMID:  14769241     Owner:  NLM     Status:  MEDLINE    
A new synthetic approach to the 1,2,5-oxadiazine ring system is described. 2-Substituted or 2,4-disubstituted 2H-1,2,5-oxadiazine-3,6(4H,5H)-dione derivatives 4 were prepared by cyclisation of hydroxamic acids 3 derived from N-(1-benzotriazolylcarbonyl)-amino acids 1. The structures of the synthesised compounds were fully characterised by IR, 1H and 13C NMR spectroscopy and elemental analysis. The aim of this study was to evaluate biological activity of the newly synthesised oxadiazine derivatives. Cytotoxic and cytostatic activities were tested on two cell lines (HeLa and GMK) and evaluated by MTT-test. Two human DNA viruses (adenovirus 7 and herpesvirus 1) and two human RNA viruses (coxsackievirus B5 and echovirus 7) were used in the antiviral test. Selected biological studies indicated that 2-phenyl- -2H-1,2,5-oxadiazine-3,6(4H,5H)-dione (4a) and 4-benzyl-2-phenyl-2H-1,2,5-oxadiazine-3,6(4H,5H)-dione (4c) statistically significantly inhibited cell growth. A minor antiviral effect was observed upon adenovirus, herpesvirus and enteroviruses.
Monika Barbarić; Sandra Kraljević; Magdalena Grce; Branka Zorc
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Acta pharmaceutica (Zagreb, Croatia)     Volume:  53     ISSN:  1330-0075     ISO Abbreviation:  Acta Pharm     Publication Date:  2003 Sep 
Date Detail:
Created Date:  2004-02-10     Completed Date:  2004-03-15     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9303678     Medline TA:  Acta Pharm     Country:  Croatia    
Other Details:
Languages:  eng     Pagination:  175-86     Citation Subset:  IM    
Faculty of Pharmacy and Biochemistry, University of Zagreb, Zagreb, Croatia.
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MeSH Terms
Antiviral Agents / chemical synthesis,  pharmacology
Cercopithecus aethiops
Hela Cells
Oxadiazoles / chemical synthesis*,  pharmacology*
Reg. No./Substance:
0/Antiviral Agents; 0/Oxadiazoles

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