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Title: Design and synthesis of cyclic sulfonamides and sulfamates as new calcium sensing receptor agonists. Author: Kiefer L, Gorojankina T, Dauban P, Faure H, Ruat M, Dodd RH. Journal: Bioorg Med Chem Lett; 2010 Dec 15; 20(24):7483-7. PubMed ID: 21041081. Abstract: The design, synthesis and calcimimetic properties of various cyclic sulfonamides and sulfamates are described. The latter were prepared from the corresponding o-alkenylarenesulfonamides via copper- or rhodium-catalyzed intramolecular aziridination. The size of the cyclic sulfonamide rings as well as the position of the crucial (R)-naphthylethylamine substituent significantly affected calcimimetic activity. The most active compounds were the six- and seven-membered sulfonamides 30a and 31a and sulfamate 34a.[Abstract] [Full Text] [Related] [New Search]