氨基哌啶吲唑类化合物作为口服有效的促黑素聚集激素受体-1拮抗剂。
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
作者信息
Vasudevan Anil, Souers Andrew J, Freeman Jennifer C, Verzal Mary K, Gao Ju, Mulhern Mathew M, Wodka Derek, Lynch John K, Engstrom Kenneth M, Wagaw Seble H, Brodjian Sevan, Dayton Brian, Falls Doug H, Bush Eugene, Brune Michael, Shapiro Robin D, Marsh Kennan C, Hernandez Lisa E, Collins Christine A, Kym Philip R
机构信息
Metabolic Diseases Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5293-7. doi: 10.1016/j.bmcl.2005.08.049. Epub 2005 Oct 3.
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
报道了新型3-氨基吲唑黑色素浓集激素受体-1拮抗剂的合成及生物学评价，其中几种拮抗剂的功能活性小于100nM。化合物19和28是本研究中鉴定出的两种活性更强的化合物，其特点是在脑中的暴露量高，并且在给饮食诱导的肥胖小鼠给药时显示出强大的功效。
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