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Synthesis of Combinatorial Libraries Based On Terpenoid Scaffolds

机译：基于萜类支架的组合库的合成

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Triterpenoid-based scaffolds betulinic acid (1a) and ursolic acid (1b), have been used for the generation of combinatorial libraries in parallel format using solid phase organic synthesis method. These templates have the potential for the synthesis and amplification of triterpenoid-based compounds with one and two-point diversity. This has been demonstrated by the synthesis of two small libraries comprising 18 derivatives each of betulinic acid and ursolic acid with structural diversity at C-3 and C-28 positions. The primary screening of antimalarial activity of these libraries against P. falciparum in vitro led to the identification of four compounds with 5 fold increase in the activity compared to betulinic and ursolic acids.
机译：基于三萜的支架，桦木酸（1a）和熊果酸（1b）已用于通过固相有机合成方法以平行形式生成组合文库。这些模板具有合成和扩增具有一点和两点多样性的三萜类化合物的潜力。通过合成两个小的文库已证明了这一点，这些文库包含18种衍生物，分别为桦木酸和熊果酸，在C-3和C-28位置具有结构多样性。这些文库对恶性疟原虫的体外抗疟活性的初步筛选导致鉴定出四种化合物，其活性与桦木酸和熊果酸相比增加了5倍。

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