Generation of a new class of hNK₂ receptor ligands using the aaafragment approachaaa

详细信息    查看全文

• 作者：DaaaAndrea ; Piero ; Porcelloni ; Marina ; Madami ; Andrea ; Patacchini ; Riccardo ; Altamura ; Maria ; et. al.
• 关键词：NK₂ ; Fragment approach
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：February 1, 2005
• 年：2005
• 卷：15
• 期：3
• 页码：585-588
• 全文大小：399 K

文摘

The so called aaafragment approachaaa was applied in the search for new leads as selective hNK₂ antagonists. A first round of structural space exploration through the use of bond rigidity as scaffold to support the fragments, afforded 27a as 200nM hNK₂ ligand. Further refinement gave MEN 14933 as a 16nM hNK₂ ligand, selective versus hNK₁, of a novel class. Conformational analysis was used to study results and plan future work.