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Synthesis and antibacterial evaluation of macrocyclic diarylheptanoid derivatives.

ABSTRACT: Bacterial infections, caused by Mycobacterium tuberculosis and other problematic bacterial pathogens, continue to pose a significant threat to global public health. As such, new chemotype antibacterial agents are desperately needed to fuel and strengthen the antibacterial drug discovery and development pipeline. As part of our antibacterial research program to develop natural product-inspired new antibacterial agents, here we report synthesis, antibacterial evaluation, and structure-activity relationship studies of an extended chemical library of macrocyclic diarylheptanoids with diverse amine, amide, urea, and sulfonamide functionalities. Results of this study have produced macrocyclic geranylamine and 4-fluorophenethylamine substituted derivatives, exhibiting moderate to good activity against M. tuberculosis and selected Gram-positive bacterial pathogens.

SUBMITTER: Lin H

PROVIDER: S-EPMC4969171 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature

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Synthesis and antibacterial evaluation of macrocyclic diarylheptanoid derivatives.

Lin Hao H Bruhn David F DF Maddox Marcus M MM Singh Aman P AP Lee Richard E RE Sun Dianqing D

Bioorganic & medicinal chemistry letters 20160627 16

Bacterial infections, caused by Mycobacterium tuberculosis and other problematic bacterial pathogens, continue to pose a significant threat to global public health. As such, new chemotype antibacterial agents are desperately needed to fuel and strengthen the antibacterial drug discovery and development pipeline. As part of our antibacterial research program to develop natural product-inspired new antibacterial agents, here we report synthesis, antibacterial evaluation, and structure-activity rel ...[more]

PMID: 27406794

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