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1,2,4-三取代哌嗪的合成及其抗结核活性

Synthesis and antitubercular activity of 1,2,4-trisubstitued piperazines.

作者信息

Rohde Kyle H, Michaels Heather A, Nefzi Adel

机构信息

University of Central Florida, College of Medicine, Burnett School of Biomedical Sciences, 6900 Lake Nona Blvd, Orlando, FL 32827, United States.

Torrey Pines Institute for Molecular Studies, Port St. Lucie, FL 34987, United States.

出版信息

Bioorg Med Chem Lett. 2016 May 1;26(9):2206-9. doi: 10.1016/j.bmcl.2016.03.063. Epub 2016 Mar 16.

DOI:10.1016/j.bmcl.2016.03.063
PMID:27020522
Abstract

Parallel solid phase synthesis offers a unique opportunity for the synthesis and screening of large numbers of compounds and significantly enhances the prospect of finding new leads. We report the synthesis and antitubercular activity of chiral 1,2,4-trisubstituted piperazines derived from resin bound acylated dipeptides against Mycobacterium tuberculosis strain H37Rv.

摘要

平行固相合成法为大量化合物的合成与筛选提供了独特的契机,并显著提升了发现新先导化合物的前景。我们报道了从树脂结合的酰化二肽衍生而来的手性1,2,4-三取代哌嗪对结核分枝杆菌H37Rv菌株的合成及抗结核活性。

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