Ontology highlight
ABSTRACT:
SUBMITTER: Guo L
PROVIDER: S-EPMC5150677 | biostudies-literature | 2016 Dec
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20161012 12
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound <b>4</b> suffered from poor metabolic stability and poor solubility. Lead optimization strategies to improve potency, efficacy, metabolic stability, and solubility are described. This optimization led to compound <b>20e</b>, which showed significant ...[more]