Fig. 31
From: The past, present and future of anti-malarial medicines
Key stages in the hit to lead pathway of DSM265. Replacement of the second phenyl ring in the naphthyl group with a trifluoromethyl group improved solubility. Addition of a 1,1-difluoroethyl group significantly increased the potency and final replacement of the trifluoromethyl group in D′2 with a pentafluorosulfur moiety led to the optimized compound DSM265