486994-14-3Relevant articles and documents
TRPV-1 RECEPTOR ANTAGONIST COMPOUND DERIVED FROM 1,3,4-THIADIAZOLE ALKYLAMIDES AND CHALCONES
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Paragraph 0031, (2015/11/11)
This technology encompasses compounds derived from 1, 3, 4-thiadiazole alkylamides and chalcone, which inhibit the activation of the TRPV-1 receptor using capsaicin and temperature. Also disclosed is the use of these compounds in the treatment of diseases with TRPV-1 overexpression, such as chronic pain.
Design and synthesis of conformationally restricted capsaicin analogues based in the 1, 3, 4-thiadiazoleheterocycle reveal a novel family of transient receptor potential vanilloid 1 (TRPV1) antagonists
Rebolledo, Carolyne Lespay,Sotelo-Hitschfeld, Pamela,Brauchi, Sebastián,Olavarría, Miguel Zárraga
, p. 193 - 203 (2013/10/01)
4-hydroxy-3-methoxybenzaldehyde was used as starting material to obtain a number of 1, 3, 4-thiadiazole alkylamide derivatives. The pharmacological properties of these conformationally restricted capsaicin analogues were evaluated on HEK-293T cells transiently expressing TRPV1 receptor. By means of a highthroughput calcium imaging assay we find that 1, 3, 4-thiadiazoles (compounds 8-15) act as potent antagonists of the capsaicin receptor, inhibiting both, the capsaicin- and temperature-dependent activation. Docking studies suggested a different binding orientation on the vanilloid binding site when compared with capsaicin analogues, such as 5-iodononivamide. Overall, our studies suggest that 1, 3, 4-thiadiazoles interact with capsaicin 's binding region of the receptor, although using a different set of interactions within the vanilloid binding pocket.
BENZO(b)FURAN DIMERS
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Page 22, (2010/02/06)
Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for