在平行阵列中使用多种反应条件对一种ICE抑制剂合成进行快速优化。
Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array.
作者信息
Warmus J S, Ryder T R, Hodges J C, Kennedy R M, Brady K D
机构信息
Department of Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 1998 Sep 8;8(17):2309-14. doi: 10.1016/s0960-894x(98)00418-1.
Optimization of a 2-step reaction sequence was accomplished in 3-4 days, with over 200 different reaction conditions evaluated. Combinatorial arrays were performed using the optimized conditions to synthesize 590 new compounds which were tested for inhibition against N-His (D381E) ICE. Thirty-five compounds showed at least a tenfold improvement in activity compared to an initial standard.
两步反应序列的优化在3至4天内完成，评估了200多种不同的反应条件。使用优化条件进行组合阵列以合成590种新化合物，并测试它们对N-His (D381E) ICE的抑制作用。与初始标准相比，有35种化合物的活性至少提高了10倍。
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