Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents

We have successfully identified a number of novel MTP inhibitors with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay.

Graphical abstractStructure activity relationship (SAR) studies of a novel class of MTP inhibitors are described. A number of novel MTP inhibitors have been identified with single digit nanomolar potency. Analogues 10aq and 10dq demonstrated in vivo efficacy in a murine gut retention assay.Figure optionsDownload full-size imageDownload as PowerPoint slide