基于 2-联苯乙基咪唑的杂环羧酸类同系物的合成及构效关系研究作为肥胖症治疗的囊泡相关膜蛋白受体 3（BRS-3）激动剂。
Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
机构信息
AMRI, 26 Corporate Circle, Albany, NY 12212, USA.
出版信息
Bioorg Med Chem Lett. 2010 May 1;20(9):2912-5. doi: 10.1016/j.bmcl.2010.03.028. Epub 2010 Mar 12.
PMID:20347296
Abstract
SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described.
摘要
呈现了非肽类强效蛙皮素受体亚型 3（BRS-3）激动剂先导 2 的 SAR 研究结果。描述了尝试用杂环等排体替代羧酸以提高口服生物利用度和脑穿透性的努力。
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