An innovative and efficient reagent- and scaffold-based diversity oriented synthesis (DOS) of a fragment set was developed for fragment-based drug discovery (FBDD) programs. Twelve diverse, functionalized and bicyclic scaffolds were rapidly accessed by adopting a convenient synthetic toolkit around three privileged azine cores in order to effectively modulate biomolecules. These structures are characterized by both key motifs for interacting with diverse biological targets via hydrogen bonds and useful points of growth for subsequent fragment optimization.

中文翻译：

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含有特权吖嗪的双环片段的多样性导向合成

为基于片段的药物发现 (FBDD) 计划开发了一种创新且高效的基于试剂和支架的片段集的多样性导向合成 (DOS)。通过围绕三个优先的吖嗪核心采用方便的合成工具包，可以快速访问十二种不同的功能化双环支架，以有效调节生物分子。这些结构的特征在于通过氢键与不同生物靶标相互作用的关键基序和用于后续片段优化的有用生长点。