Given the relevance of the DPP IV/CA (II andV) roles in both T2DM and obesity, multitarget ligands able to modulatethese enzymes could represent a novel and promising therapeutic approach.Repositioning of WB-4101 and morphing its structure have been thestrategies applied to obtain potent and selective multitarget ligandsagainst DPP IV and CAs (isoforms II and V). Here, DPP4 is linked to type 2 diabetes mellitus.