4.7 Article

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

期刊

JOURNAL OF NATURAL PRODUCTS
卷 77, 期 8, 页码 1972-1975

出版社

AMER CHEMICAL SOC
DOI: 10.1021/np500281c

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资金

  1. Sao Paulo Research Foundation (FAPESP) [06/61187-7, 03/00886-7, 2011/51313-3]
  2. CNPq
  3. CAPES
  4. FAPESP
  5. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [06/61187-7, 03/00886-7] Funding Source: FAPESP

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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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