Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo(1,5-a)pyrimidines as novel PDE-4 inhibitors.

Kim I; Song JH; Park C

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo(1,5-a)pyrimidines as novel PDE-4 inhibitors.

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Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo(1,5-a)pyrimidines as novel PDE-4 inhibitors.

机译：设计，合成和评估2-芳基-7-（3'，4'-二烷氧基苯基）-吡唑并（1,5-a）嘧啶作为新型PDE-4抑制剂。

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Described herein is design, synthesis, and biological evaluation of novel series of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines acting as inhibitors of type 4 phosphodiesterase (PDE4) which is known as a good target for the treatment of asthma and COPD. For this purpose, structure optimization was conducted with the aid of structure-based drug design using the known X-ray crystallography. Also, biological effects of these compounds on the target enzyme were evaluated by using in vitro assays, leading to the potent and selective PDE-4 inhibitor (IC(50)<10nM).

机译：本文描述了新颖的2-芳基-7-（3'，4'-二烷氧基苯基）-吡唑并[1,5-a]嘧啶系列的新颖系列的设计，合成和生物学评估，该抑制剂可作为4型磷酸二酯酶（PDE4）的抑制剂被认为是治疗哮喘和COPD的好靶标。为此目的，使用已知的X射线晶体学，借助于基于结构的药物设计进行结构优化。此外，通过使用体外测定法评估了这些化合物对目标酶的生物学作用，从而产生了有效且选择性的PDE-4抑制剂（IC（50）<10nM）。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共5页
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Kim I; Song JH; Park C;
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1. Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo(1,5-a)pyrimidines as novel PDE-4 inhibitors. [J] . Kim I, Song JH, Park C Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：设计，合成和评估2-芳基-7-（3'，4'-二烷氧基苯基）-吡唑并（1,5-a）嘧啶作为新型PDE-4抑制剂。
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Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo(1,5-a)pyrimidines as novel PDE-4 inhibitors.

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