Facile synthesis, antibacterial and protease inhibition studies of beta-amino alcohols prepared via ring opening of epoxides

PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES(2022)

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摘要
A green ultrasound assisted convenient approach has been reported for the ring opening of epoxides. As a result, a series of N-phenyl piperazine and morpholine based 13-amino alcohols has been synthesized under ultrasound irradiation in DMSO for 60 minutes at 70 degrees C. This methodology showed excellent tolerance with various epoxides and provided excellent yields upto 96%. All the synthetic derivatives (4a-e) (5c-d) significantly influence the catalytic activity of protease while 5d exhibited maximum (100%) inhibitory effect with a half-life of 40.76 minutes. Among the target derivatives, compound 4c exhibited significant antibacterial activity against Bacillus subtilis and Escherichia coli bacterial strains with zone of inhibition values 45 mm and 32 mm, respectively.
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关键词
Epoxide ring opening, N-phenyl piperazine, amino alcohols, protease, epoxides, antibacterial activity
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