Ballell Lluis, Field Robert A, Chung Gavin A C, Young Robert J
Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK.
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1736-40. doi: 10.1016/j.bmcl.2006.12.066. Epub 2006 Dec 22.
The multiple parallel synthesis of a series of N,S-bis-alkylated thiopyrazolo[3,4-d]pyrimidines, based on sequential S- then N-alkylation, is reported. These compounds showed significant anti-mycobacterial activity (MICs down to 2mug/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling.
报道了基于先后进行S-烷基化和N-烷基化的一系列N,S-双烷基化硫代吡唑并[3,4-d]嘧啶的多平行合成。这些化合物显示出显著的抗分枝杆菌活性（最低MIC值达2μg/ml），并且通过细胞毒性评估和计算机模拟分析证实了它们作为具有显著药物样特性先导物的潜力。
