期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 22, 页码 6888-6895出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.09.059
关键词
Vanilloid receptor; Ligand-gated ion channel; TRPV1; Pain; Indolizine; Pyrrolopyridazine
A novel indolizine class of compounds was identified as TRPV1 antagonist from an HTS campaign. However, this indolizine class proved to be unstable and reacted readily with glutathione when exposed to light and oxygen. Reactivity was reduced by the introduction of a nitrogen atom alpha to the indolizine nitrogen. The pyrrolopyridazine core obtained proved to be inert to the action of light and oxygen. The synthesis route followed the one used for the indolizine compounds, and the potency and ADMET profile proved to be similar. (C) 2012 Elsevier Ltd. All rights reserved.
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