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Design, synthesis and biological evaluation of non-hydrolyzable phosphate mimetics of receptor subtype selective LPA antagonists.

机译：受体亚型选择性LPA拮抗剂的不可水解磷酸盐模拟物的设计，合成和生物学评估。

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摘要

Lysophosphatidic acid (LPA) is an endogenous lysophospholipid that is generated by a variety of cell types. It is thought to be responsible for eliciting numerous biological responses of significant importance. These include wound healing, cancer progression, atherogenesis and neoplasia. LPA causes its biological effects by acting upon a family of G-coupled protein receptors (GPCRs) formerly known as Endotheilial differentiation gene (Edg) receptors. These receptors are now referred to as simply LPA receptors. There are currently 4 extracellular LPA receptors which include LPA1 (formerly Edg2), LPA2 (formerly Edg4), LPA3 (formerly Edg7) and LPA 4 that was recently de-orphaned (formerly GPR23) and one intracellular receptor PPARgamma. Recently we have described a subtype selective antagonist for the LPA1 and LPA3 receptors based on the N-acyl ethanol amide phosphoric acid (NAEPA) moiety. This work describes the synthetic efforts used to make non-hydrolyzable alpha and beta substituted phosphonate analogs of NAEPA; as well as carboxylic acid analogs of NAEPA. The structure activity relationship profile of these unique compounds will also be discussed.
机译：溶血磷脂酸（LPA）是由多种细胞类型产生的内源性溶血磷脂。认为引起大量重要的生物学反应是有原因的。这些包括伤口愈合，癌症进展，动脉粥样硬化和瘤形成。 LPA通过作用于以前称为内皮分化基因（Edg）受体的G偶联蛋白受体（GPCR）家族而引起其生物学效应。这些受体现在简称为LPA受体。当前有4种细胞外LPA受体，包括LPA1（以前称为Edg2），LPA2（以前称为Edg4），LPA3（以前称为Edg7）和最近被孤立的LPA 4（以前称为GPR23）和一种细胞内受体PPARgamma。最近，我们已经描述了基于N-酰基乙醇酰胺磷酸（NAEPA）部分的LPA1和LPA3受体的亚型选择性拮抗剂。这项工作描述了用于制备不可水解的αEPA和β取代的NAEPA膦酸酯类似物的合成方法。以及NAEPA的羧酸类似物。这些独特化合物的结构活性关系图也将进行讨论。

著录项

  • 作者

    McCalmont, William Forest.;

  • 作者单位

    University of Virginia.;

  • 授予单位 University of Virginia.;
  • 学科 Chemistry Organic.; Chemistry Pharmaceutical.
  • 学位 Ph.D.
  • 年度 2006
  • 页码 171 p.
  • 总页数 171
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 有机化学;药物化学;
  • 关键词

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