Molecules (2016)
Update date:2022-07-30
Topics: Synthesis Antibacterial Antimicrobial Characterization NMR spectroscopy Derivatives Microwave irradiation Alkaloid Synthesize Experimental
Zheng, Shaojun
Zhou, Xinping
Xu, Shixun
Zhu, Rui
Bai, Hongjin
Zhang, Jiwen
A total of 29 novel tetrahydropyrroloindol-based calycanthaceous alkaloid derivatives were synthesized from indole-3-acetonitrile in good yields. The synthesized compounds were evaluated against nine strains of bacteria and a wide range of plant pathogen fungi. Bioassay results revealed that majority of the compounds displayed similar or higher in vitro antimicrobial activities than the positive control. The biological activities also indicated that substituents at R4 and R5 significantly affect the activities. Notably, compound c4 was found to be most active among the tested calycanthaceous analogues and might be a novel potential leading compound for further development as an antifungal agent. The results could pave the way for further design and structural modification of calycanthaceous alkaloids as antimicrobial agents.
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