作为生物活性分子来源的类肽位置扫描组合文库：抗菌剂的鉴定。
A positional scanning combinatorial library of peptoids as a source of biological active molecules: identification of antimicrobials.
作者信息
Humet Marc, Carbonell Teresa, Masip Isabel, Sánchez-Baeza Francisco, Mora Puig, Cantón Emilia, Gobernado Miguel, Abad Concepción, Pérez-Payá Enrique, Messeguer Angel
机构信息
Department of Biological Organic Chemistry, I.I.Q.A.B. (C.S.I.C.), E-08034 Barcelona, Spain.
出版信息
J Comb Chem. 2003 Sep-Oct;5(5):597-605. doi: 10.1021/cc020075u.
A positional scanning library of N-alkylglycine trimers (peptoids) containing over 10 000 compounds has been synthesized on solid phase. The synthetic pathway involved the use of the submonomer strategy and a set of 22 commercially available primary amines as a chemical diversity source. The unbiased nature of the library allowed its screening against a variety of biological targets, leading to the identification of individual peptoids exhibiting remarkable biological activities (García-Martínez, C. et al. Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 2374. Montoliu, et al. J. Pharm. Exp. Therap. 2002, 302, 29. Planells-Cases, R., et al. J. Pharm. Exp. Therap. 2002, 302, 163). In the present work, the screening of this library against a panel of Gram-positive and Gram-negative bacteria led to the identification of different compounds exhibiting antimicrobial activity.
已在固相上合成了一个包含超过10000种化合物的N-烷基甘氨酸三聚体（类肽）的位置扫描文库。合成途径涉及使用亚单体策略和一组22种市售伯胺作为化学多样性来源。该文库的无偏性使其能够针对多种生物靶点进行筛选，从而鉴定出具有显著生物活性的单个类肽（加西亚 - 马丁内斯，C.等人。美国国家科学院院刊2002年，99，2374。蒙托柳等人。药物实验与治疗杂志2002年，302，29。普拉内尔斯 - 卡塞斯，R.等人。药物实验与治疗杂志2002年，302，163）。在本研究中，针对一组革兰氏阳性和革兰氏阴性细菌对该文库进行筛选，从而鉴定出了具有抗菌活性的不同化合物。
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