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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Design and synthesis of an optimized positional scanning library of peptoids: identification of novel multidrug resistance reversal agents.
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Design and synthesis of an optimized positional scanning library of peptoids: identification of novel multidrug resistance reversal agents.

机译：类肽的最佳位置扫描库的设计和合成：新型多药耐药逆转剂的鉴定。

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摘要

Herein is reported the optimized solid-phase synthesis of a library of 5,120 trimeric N-alkylglycines (peptoids) using the positional scanning format and the submonomer strategy. Diversity at the N-terminal position was generated from 20 commercially available primary amines, whereas 16 primary amines were employed for the middle and C-terminal positions of the trimers. Formation of undesirable side-products observed in a previous library synthesis (Humet, M. et al. J. Comb. Chem. 2003, 5, 597-605) was averted by restricting the use of primary amines functionalized with tertiary amino groups to the third amination step. Screening of the new library for the identification of chemosensitizers yielded two peptoids, compounds 1 and 2, with potent in vitro activity as multidrug resistance (MDR) reversal agents. The structures of the lead peptoids are consistent with a pharmacophore model generated from the interaction of various known inhibitors with the MDR-implicated transmembrane glycoprotein P-gp.
机译：本文报道了使用位置扫描格式和亚单体策略对5,120个三聚N-烷基甘氨酸（类肽）的文库进行优化的固相合成。 N末端位置的多样性是由20种市售伯胺产生的，而三聚体的中间和C末端位置使用了16种伯胺。通过限制使用叔胺基官能化的伯胺，避免了在以前的文库合成中观察到的不良副产物的形成（Humet，M. et al。J. Comb。Chem。2003，5，597-605）。第三步胺化。筛选用于鉴定化学增敏剂的新文库，产生了两种类肽，化合物1和2，具有作为多药抗性（MDR）逆转剂的有效体外活性。铅类肽的结构与由各种已知抑制剂与MDR牵连的跨膜糖蛋白P-gp相互作用产生的药效团模型一致。

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