Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin.

Matthews JM; Liotta F; Hageman W; Rivero RA; Westover L; Yang M; Xu J; Demarest K

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Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin.

机译：发现选择性模拟降钙素的生物作用的二氢嘧啶系列分子。

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The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC(50)=6 microM), active in-vivo in the Weanling rat model when administered subcutaneously.

机译：多重模拟试验的使用使我们鉴定出具有有效和选择性降钙素受体模拟活性的1，4-二氢嘧啶。二氢嘧啶支架的后续修饰导致一系列分子在新生小鼠颅颅体外模型中有效。尤其是二氢嘧啶5h被确定为降钙素模拟物（EC（50）= 6 microM），在断奶大鼠模型中皮下给药时具有活体内作用。

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《Bioorganic and Medicinal Chemistry Letters》 |2004年第5期|共5页
作者
Matthews JM; Liotta F; Hageman W; Rivero RA; Westover L; Yang M; Xu J; Demarest K;
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原文格式 PDF
正文语种 eng
中图分类基础医学;
关键词
Calcitonin; Models; receptor; assay; Neon; 降钙素; 氖;

机译：Calcitonin;Models;receptor;assay;Neon;降钙素;氖;

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1. Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin. [J] . Matthews JM, Liotta F, Hageman W, Bioorganic and Medicinal Chemistry Letters . 2004,第5期

机译：发现选择性模拟降钙素的生物作用的二氢嘧啶系列分子。
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Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin.

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