N-Isoquinolin-5-yl-N′-aralkyl-urea and -amide Antagonists of Human Vanilloid Receptor 1.

Johnson & Johnson Pharmaceutical Research and Development, Welsh and McKean Roads, Spring House, PA 19477, USA.
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.42). 07/2004; 14(12):3053-6. DOI: 10.1016/j.bmcl.2004.04.038
Source: PubMed


Starting from a low micromolar agonist lead identified by high-throughput screening, series of N-isoquinolin-5-yl-N'-aralkyl ureas and analogous amides were developed as potent antagonists of human vanilloid receptor 1 (VR1). The synthesis and structure-activity relationships (SAR) of the series are described.

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