Synthetic utility of sydnones: synthesis of pyrazolines derivatized with 1,2,4-triazoles as antihyperglymic, antioxidant agents and their DNA cleavage study
Ring transformation of sydnone ( 1a – i ) to 1,3,4-oxadiazoline-2-one ( 2a – i ) was carried out using bromine in acetic anhydride. The compounds ( 2a – i ) on heating with hydrazine hydrate gave 1,2,4-triazole ( 3a – i ) in good yields. The structure of these unknown compounds was confirmed by IR,...
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Veröffentlicht in: | Medicinal chemistry research 2012-11, Vol.21 (11), p.3709-3719 |
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Hauptverfasser: | , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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Zusammenfassung: | Ring transformation of sydnone (
1a
–
i
) to 1,3,4-oxadiazoline-2-one (
2a
–
i
) was carried out using bromine in acetic anhydride. The compounds (
2a
–
i
) on heating with hydrazine hydrate gave 1,2,4-triazole (
3a
–
i
) in good yields. The structure of these unknown compounds was confirmed by IR,
1
H NMR, MS and elemental analysis. Further, these compounds were evaluated for the extent of penetration into biological membranes (clog
P
) drug likeliness and finally drug score was calculated. The title compounds were also screened for their antihyperglycemic, DNA cleavage and antioxidant activity. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-011-9921-9 |