Discovery of a series of potent arylthiadiazole H(3) antagonists.
Discovery of a series of potent arylthiadiazole H(3) antagonists.
复制标题
发现一系列有效的芳基噻二唑 H(3) 拮抗剂。
DOI：
10.1016/j.bmcl.2010.11.065
复制
发表时间：
2011
影响因子：
2.7
通讯作者：
J. Lachowicz
中科院分区：
文献类型：
--
作者：
D. Xiao;A. Palani;Michael Sofolarides;Ying Huang;R. Aslanian;H. Vaccaro;L. Hong;B. Mckittrick;R. West;S. M. Williams;R. Wu;Joyce Hwa;Christopher Sondey;J. Lachowicz
合成了一系列2-哌啶基哌啶-5-芳基噻二唑类化合物，并对其构效关系进行了研究。该系列的效力提高至个位数纳摩尔范围。关键的类似物被证明没有P450问题，并且它们还保持了良好的离体活性和脑渗透。
A series of 2-piperidinopiperidine-5-arylthiadiazoles was synthesized and subjected to a structure–activity relationship (SAR) investigation. The potency of this series was improved to the single digit nanomolar range. The key analogs were shown to be free of P450 issues, and they also maintained good ex vivo activity and brain penetration.