Design, Synthesis, Physical Properties and Indoleamine 2, 3-Dioxygenase 1 Inhibitory Activity of Substituted Indole Derivatives with N-H, N-Methoxymethyl, or N-Mehylthiomethyl Group toward Fragment-Based Drug Discovery

Abstract

We designed and prepared N-H, N-CH2OMe (MOM), and N-CH2SMe (MTM) forms of various substituted indoles, using a docking study, as a small fragment library toward fragment-based drug discovery (FBDD) and evaluated their indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitory activities and physical properties.