Synthesis and in vitro study of methylene-bis-tetrahydro[1,3]thiazolo[4,5- c]isoxazoles as potential nematicidal agents
A series of methylene-bis-tetrahydro[1,3]thiazolo[4,5- c]isoxazoles 6 were synthesized by the reaction of chalcone derivative of methylene-bis-thiazolidinone 5 with hydroxylamine hydrochloride. The chemical structures of newly synthesized compounds were elucidated by IR, 1H, 13C NMR, MS and elementa...
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Published in | European journal of medicinal chemistry Vol. 45; no. 6; pp. 2353 - 2358 |
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Main Authors | , , |
Format | Journal Article |
Language | English |
Published |
ISSY-LES-MOULINEAUX
Elsevier Masson SAS
01.06.2010
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A series of methylene-bis-tetrahydro[1,3]thiazolo[4,5-
c]isoxazoles
6 were synthesized by the reaction of chalcone derivative of methylene-bis-thiazolidinone
5 with hydroxylamine hydrochloride. The chemical structures of newly synthesized compounds were elucidated by IR,
1H,
13C NMR, MS and elemental analyses. The compounds
6a–
g were evaluated for their nematicidal activity against
Ditylenchus myceliophagus and
Caenorhabditis elegans, compound
6e and
6f showed appreciable nematicidal activity. Further the compounds
6a–
g were screened for their antifungal activity against
Candida albicans (ATCC 10231),
Aspergillus fumigatus (HIC 6094),
Trichophyton rubrum (IFO 9185) and
Trichophyton mentagrophytes (IFO 40996). The compounds
6b and
6f displayed notable antifungal activity against all the microorganisms employed. The activity of these two compounds is almost equal to the standard. It is also interesting to note that the compounds
6b,
6f and
6g showed activity towards
C. albicans at the concentration of 3.75 μM, which is less than the concentration of the standard Amphotericin B.
A series of methylene-bis-tetrahydro[1,3]thiazolo[4,5-
c]isoxazoles have been synthesized and screened for their
in vitro antifungal and nematicidal activities.
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2010.02.014 |