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United States Department of Agriculture

Agricultural Research Service

Research Project: DISCOVERY AND DEVELOPMENT OF NATURAL PRODUCT FOR PHARMACEUTICAL AND AGRICHEMICAL APPLICATIONS Title: Natural product-based 6-hydroxy-2 3 4 6-tetrahydropyrrolo[1 2-a]pyrimidinium Scaffold as a new antifungal template

item Li, Xing-Cong -
item Babu, K. Suresh -
item Jacob, Melissa -
item Khan, Shabana -
item Agarwal, Ameeta -
item Clark, Alice -

Submitted to: ACS Medicinal Chemistry Letters
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: March 14, 2011
Publication Date: March 18, 2011
Citation: Li, X., Babu, K., Jacob, M.R., Khan, S.I., Agarwal, A.K., Clark, A.M. 2011. Natural product-based 6-hydroxy-2,3,4,6-tetrahydropyrrolo[1,2-a]pyrimidinium scaffold as a new antifungal template. ACS Medicinal Chemistry Letters. 2:391-395.

Interpretive Summary: The manuscript describes the isolation of antifungal phloeodictine alkaloids from the marine sponge Pellina eusiphonia and subsequent synthesis of analogs that demonstrated potent antifungal activity.

Technical Abstract: Synthetic analogues of the marine-derived class of natural products phloeodictines have been prepared and exhibited potent in vitro fungicidal activities against a broad array of fungal pathogens including drug-resistant strains. The 6-hydroxy-2,3,4,6-tetrahydropyrrolo[1,2-a] pyrimidinium structural moiety with a C12 to C16 aliphatic side chain at C-6 has been shown to be the antifungal pharmacophore and may serve as a new antifungal template for further lead optimization.

Last Modified: 8/4/2015
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