Synthesis and Biological Studies of Bis-Heterocycles
Corresponding Author(s) : S.M. Kudari
Asian Journal of Chemistry,
Vol. 9 No. 1 (1997): Vol 9 Issue 1
Abstract
Reaction of succinic acid hydrazide with substituted isothiocyanate
gave corresponding thiosemicarbazides (IIa–c) in good
yields. The acid catalysed cyclodehydration of (IIa) gave corresponding
oxadiazole (Va). The base catalysed cyclodehydration of
(IIa–c) gave respective bis-triazoles (IIIa–c) and cylisation of (IIa–c)
with 99% hydrazine hydrate gave respective N-amino triazoles
(VIa–c). Reaction of oxalic acid hydrazide with CS2/KOH gave the
corresponding salt (VI). Cyclisation of (VI) with hyrazine hydrate
and phenyl hydrazine hydrate gave corresponding 4-substituted bis-triazoles
(VIIa–b). Treatment of (VI) with CH3I/CH3OH gave the
methyl salt (VIII). Prolonged refluxing of (VI) with KOH/
C2H5OH gave bis-5-mercapto-1,2,4-oxadiazole (IX).Treatrnent of
substituted benzoic acid with acid hydrazide in presence of
POCl3 yielded 5-substituted oxadiazole (Xa–b). Sample number
Xa–b on cyclisation with hydrazine hydrate and phenyl hydrazine
hydrate gave (XIa–d). Potassium salt (VI) on treating with substituted
aniline gave (XIIa–b). All the above compounds are
screened for antimicrobial and anthelmintic activities. They showed
moderate to high activity.
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