Li Xing-Cong, Babu K Suresh, Jacob Melissa R, Khan Shabana I, Agarwal Ameeta K, Clark Alice M
National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, University of Mississippi, University, Mississippi 38677.
ACS Med Chem Lett. 2011 May 12;2(5):391-395. doi: 10.1021/ml200020h.
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.
已经制备了源自海洋的天然产物类叶苦定碱的合成类似物，它们对包括耐药菌株在内的多种真菌病原体表现出强大的体外杀菌活性。已证明在C-6位带有C12至C16脂肪族侧链的6-羟基-2,3,4,6-四氢吡咯并[1,2-a]嘧啶鎓结构部分是抗真菌药效基团，可作为进一步优化先导化合物的新抗真菌模板。
