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新型吡啶并嘧啶衍生物作为稳定毒素a(STa)诱导的cGMP合成抑制剂

Novel pyridopyrimidine derivatives as inhibitors of stable toxin a (STa) induced cGMP synthesis.

作者信息

Tanifum Eric A, Kots Alexander Y, Choi Byung-Kwon, Murad Ferid, Gilbertson Scott R

机构信息

Department of Pharmacology and Toxicology, The University of Texas Medical Branch, Galveston, TX 77555-0650, USA.

出版信息

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3067-71. doi: 10.1016/j.bmcl.2009.04.024. Epub 2009 Apr 12.

Abstract

A series of pyridopyrimidine derivatives were synthesized and evaluated for their ability to inhibit cyclic nucleotide synthesis in the presence of stable toxin a of Escherichia coli. The structure activity relationships around the basic core structure were examined and examples with better activity and potentially better pharmacological properties are presented.

摘要

合成了一系列吡啶并嘧啶衍生物,并评估了它们在存在大肠杆菌稳定毒素a的情况下抑制环核苷酸合成的能力。研究了围绕基本核心结构的构效关系,并给出了具有更好活性和潜在更好药理特性的实例。

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