DESIGN, SYNTHESIS AND ANTIMICROBIAL EVALUATION OF SOME MANNICH BASE DERIVATIVE OF 2-(SUBTITUTED)-5-AMINO-THIADIAZOLES
Objective: The major objective of the present study was to design, synthesize some Mannich base derivative of 2-substituted-5-amino thiadiazoles with primary amines/phthalimide and formaldehyde anticipating effective as antimicrobial agents.
Methods: The efficient syntheses of substituted thiadiazole were done simply by reaction of substituted benzoic acid with thiosemicarbazide in presence of only conc. sulphuric acid. The isolated products were further subjected for Mannich reaction and evaluated for antibacterial activity.
Results: Three substituted thiadiazoles (BA-1 to BA-3) were synthesized by solvent less efficient synthesis and their Mannich base derivates were also prepared with phthalimide, p-nitro/methyl/chloro-aniline. All characterized products were screened for antibacterial and antifungal activities. Among these compounds having nitro group (3,7,13) showed maximum activity followed by phthalimide, chloro and methyl groups.
Conclusion: Thiadiazole-Mannich bases derivatives exhibited better antimicrobial activities then their starting components (BA-1 to BA-3) indicated joining different pharmacophore in the same molecule have increased activity.
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