Discovery and SAR of cyclic isothioureas as novel NPY Y₁ receptor antagonists

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• 作者：Zhong-Yue Sun ; Zhaoning Zhu ; Yuanzan Ye ; Brian McKittrick ; Michael Czarniecki ; William Greenlee ; Deborra Mullins ; Mario Guzzi
• 关键词：NPY Y₁ receptor antagonist ; Thioisourea ; Thiazoline ; Thiazine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 December 2009
• 年：2009
• 卷：19
• 期：23
• 页码：6801-6805
• 全文大小：568 K

文摘

A class of novel 2-aminobenzothiazoles have been identified as NPY Y₁ antagonists. Various N-heterocyclic substituted aminophenethyl-2-aminobenzothiazole analogs were synthesized to explore the SAR. Isothiourea analogs and ligands with high potency (K_i 30 nM) have been identified.