N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: A Novel, Exceptionally Selective, Potent δ Opioid Receptor Agonist with Oral Bioavailability and Its Analogues was written by Wei, Zhong-Yong;Brown, William;Takasaki, Bryan;Plobeck, Niklas;Delorme, Daniel;Zhou, Fei;Yang, Hua;Jones, Paul;Gawell, Lars;Gagnon, Helene;Schmidt, Ralf;Yue, Shi-Yi;Walpole, Chris;Payza, Kemal;St-Onge, Stephane;Labarre, Maryse;Godbout, Claude;Jakob, Andrea;Butterworth, Joanne;Kamassah, Augustus;Morin, Pierre-Emmanuel;Projean, Denis;Ducharme, Julie;Roberts, Edward. And the article was included in Journal of Medicinal Chemistry in 2000.Category: iodides-buliding-blocks This article mentions the following:
The design, synthesis, and pharmacol. evaluation of a novel class of δ opioid receptor agonists, N,N-diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide (I) and its analogs, are described. These compounds, formally derived from SNC-80 by replacing the piperazine ring with a piperidine ring containing an exocyclic carbon carbon double bond, were found to bind with high affinity and exhibit excellent selectivity for the δ opioid receptor as full agonists. I, the simplest structure in the class, exhibited an IC50 = 0.87 nM for the δ opioid receptors and extremely high selectivity over the μ receptors (μ/δ = 4370) and the κ receptors (κ/δ = 8590). Rat liver microsome studies on a selected number of compounds show these olefinic piperidine compounds to be considerably more stable than SNC-80. This novel series of compounds appear to interact with δ opioid receptors in a similar way to SNC-80 since they demonstrate similar SAR. Two general approaches have been established for the synthesis of these compounds, based on dehydration of benzhydryl alcs. and Suzuki coupling reactions of vinyl bromide. In the experiment, the researchers used many compounds, for example, N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8Category: iodides-buliding-blocks).
N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Polyiodoorganic compounds are sometimes employed as X-ray contrast agents, in fluoroscopy, a type of medical imaging. This application exploits the X-ray absorbing ability of the heavy iodine nucleus.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com