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ChemInform Abstract: Synthesis of Novel Triplet Drugs with 1,3,5-Trioxazatriquinane Skeletons and Their Pharmacologies. Part 2. Synthesis of Novel Triplet Drugs with the Epoxymethano Structure (Capped Homotriplet)
- Source :
- ChemInform. 43
- Publication Year :
- 2012
- Publisher :
- Wiley, 2012.
-
Abstract
- An improved synthetic method for triplet drugs with the 1,3,5-trioxazatriquinane skeleton was developed that used p-toluenesulfonylmethyl isocyanide (TosMIC) instead of 1,3-dithiane. Using the improved method, we synthesized compounds with two identical pharmacophore units and an epoxymethano group, that is, capped homotriplets. Among the synthesized capped homotriplets, KNT-123 showed high selectivity for the μ receptor over the κ receptor, and the μ selectivity was the highest among the reported μ selective nonpeptide ligands. KNT-123 administered subcutaneously induced a dose-dependent analgesic effect in the acetic acid writhing assay, and its potency was 11-fold more potent than that of morphine. KNT-123 may serve as a useful tool for the study of the pharmacological actions mediated specifically via the μ receptor.
Details
- ISSN :
- 09317597
- Volume :
- 43
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi...........9916eff8347fd727ae507294ca991534