A discrete library of linear and hydantoin-containing dipeptide derivatives, based on the Lys-Trp(Nps) scaffold, was prepared by solid-phase synthesis. SAR studies indicated that potency for TRPV1 blockade and selectivity towards NMDA is mainly dictated by the side-chain length and the basic nature of α, ω-groups in the N-terminal residue. The 2-Nps moiety at position 2 of Trp indole ring is preferred over the 2-pyridine one.
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| http://dx.doi.org/10.1016/j.bmcl.2011.04.141 | DOI Listing |
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Article Synopsis
- TRPV channels are part of a larger superfamily and are found in many cell types, with TRPV1-4 being sensitive to temperature and TRPV5-6 being selective for calcium ions.
- These channels are important in various physiological processes and can be influenced by internal and external compounds, making them a target for pharmacological research.
- Modulating these channels is crucial because it could lead to treatments for diseases like neurodegenerative disorders, pain, cancer, and skin issues, and there has been recent progress in exploring their ligands and related pharmacological effects.
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