| 19631535 |
Simeone JP, Braun MP, Leone JF, Lin P, DeVita RJ, Garcia-Calvo M, Bull HG, Lisnock J, Dean DC: Multiple strategies for the preparation of a sulfur-35 labeled NPC1L1 radioligand. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5033-6. Epub 2009 Jul 22.
During our effort to design a receptor binding assay to aid in the elucidation of the molecular mechanism of ezetimibe, we prepared a sulfur-35 containing radioligand which exhibits improved potency over the glucuronide conjugate of ezetimibe in both native enterocyte brush border membranes and membranes from cells expressing recombinant NPC1L1. Herein, we describe the different synthetic strategies which were used to obtain this compound as well as its effectiveness in the aforementioned assay. |
87(1,1,2,2) |