2. Academic Validation
  3. In Vitro Antibacterial Activity of Prenylated Guanidine Alkaloids from Pterogyne nitens and Synthetic Analogues

In Vitro Antibacterial Activity of Prenylated Guanidine Alkaloids from Pterogyne nitens and Synthetic Analogues

  • J Nat Prod. 2014 Aug 22;77(8):1972-5. doi: 10.1021/np500281c.
Aline Coqueiro 1 2,  Luis Octávio Regasini 1,  Paul Stapleton 2,  Vanderlan da Silva Bolzani 1,  Simon Gibbons 2
Affiliations

Affiliations

  • 1 Department of Organic Chemistry, Institute of Chemistry, São Paulo State University , Rua Prof. Francisco Degni 55, Araraquara14800-900, Brazil.
  • 2 Department of Pharmaceutical and Biological Chemistry, UCL School of Pharmacy , 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
PMID: 25089583 DOI: 10.1021/np500281c
Abstract

The present investigation deals with the Antibiotic activity of eight natural guanidine Alkaloids and two synthetic analogues against a variety of clinically relevant methicillin-resistant Staphylococcus aureus strains. Galegine (1) and pterogynidine (2) were the most potent compounds, with a minimum inhibitory concentration of 4 mg/L, to all tested strains. The preliminary chemical features correlating to anti-MRSA activity showed that the size of the side chain and the substitution pattern in the guanidine core played a key role in the Antibacterial activity of the imino group. Guanidine Alkaloids 1 and 2 are promising molecular models for further synthetic derivatives and, thus, for medicinal chemistry studies.

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