2. Academic Validation
  3. The synthesis and biological evaluation of alkyl and benzyl naphthyridinium analogs of eupolauridine as potential antimicrobial and cytotoxic agents

The synthesis and biological evaluation of alkyl and benzyl naphthyridinium analogs of eupolauridine as potential antimicrobial and cytotoxic agents

  • Bioorg Med Chem. 2016 Dec 1;24(23):6119-6130. doi: 10.1016/j.bmc.2016.02.028.
Shahriyar Taghavi-Moghadam 1,  Cecil D Kwong 1,  John A Secrist 3rd 2,  Shabana I Khan 3,  Alice M Clark 3
Affiliations

Affiliations

  • 1 Organic Chemistry Department, Southern Research Institute, 2000 Ninth Avenue South, PO Box 55305, Birmingham, AL 35255, United States.
  • 2 Organic Chemistry Department, Southern Research Institute, 2000 Ninth Avenue South, PO Box 55305, Birmingham, AL 35255, United States. Electronic address: secrist@southernresearch.org.
  • 3 National Center for Natural Products Research, and Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677, United States.
PMID: 27769668 DOI: 10.1016/j.bmc.2016.02.028
Abstract

Eupolauridine, an indenonaphthyridine alkaloid, has been previously reported by us to exhibit Antifungal activity. This study describes the synthesis of new alkyl and benzyl naphthyridinium/pyridinium analogs of eupolauridine as potential Antifungal agents. A majority of the analogs exhibited Antifungal activity against opportunistic pathogens such as Candida albicans and Cryptococcus neoformans. Several of them were also effective against bacteria (Staphylococcus aureus, MRS, Pseudomonas and Mycobacterium) and the malaria Parasite (Plasmodium falciparum) to variable extents. A number of analogs were also cytotoxic to human Cancer cell lines.

Keywords

Antibacterial; Antifungal; Antimicrobial; Eupolauridine analogs.

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