2. Academic Validation
  3. Synthesis and antibacterial evaluation of macrocyclic diarylheptanoid derivatives

Synthesis and antibacterial evaluation of macrocyclic diarylheptanoid derivatives

  • Bioorg Med Chem Lett. 2016 Aug 15;26(16):4070-6. doi: 10.1016/j.bmcl.2016.06.075.
Hao Lin 1,  David F Bruhn 2,  Marcus M Maddox 2,  Aman P Singh 2,  Richard E Lee 2,  Dianqing Sun 3
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA.
  • 2 Department of Chemical Biology & Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, MS#1000, Memphis, TN 38105, USA.
  • 3 Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA. Electronic address: [email protected].
PMID: 27406794 DOI: 10.1016/j.bmcl.2016.06.075
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.

Keywords

Antibacterial; Antituberculosis; Diarylheptanoid; Macrocycle; SAR.

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