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. 2005 Oct 5;7(2):E496–E502. doi: 10.1208/aapsj070250

Further advances in the synthesis of endocannabinoid-related ligands

Anu Mahadevan 1,✉, Raj K Razdan 1
PMCID: PMC2750987  PMID: 16353927

Abstract

Recent advances in the synthesis of endocannabinoid-related ligands for the period 2001–2004 are covered in this review. During this period the first solid phase synthesis of anandamide (AEA) analogs was developed, which allows modification at both the head group and the end pentyl chain. Synthesis of water-soluble prodrugs of noladin, ether was reported, which are chemically stable, rapidly release noladin ether under enzymatic conditions and are shown to reduce intraocular pressure. The structure-activity relationships (SAR) of alkylcarbamic acid aryl esters and the discovery of potent, archidonylsulfonyl derivatives as fatty acid amide hydrolase (FAAH) inhibitors are summarized. Recent synthetic developments in the controversial area of anandamide membrane transporter (AMT) inhibitors are also discussed.

Keywords: endocannabinoids, synthesis, structure-activity relationship

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