Natural Product-Based 6-Hydroxy-2,3,4,6-tetrahydropyrrolo[1, 2-a]pyrimidinium Scaffold as a New Antifungal Template

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.