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Key stages in the hit to lead pathway of MMV253. Initial replacement of ethylbenzene on M’1 with 2-methylpyridine resulted in lower hERG affinity and improved solubility. Substitution of the pyrrolidine in M’2 with an imidazole containing an amine spacer further improved solubility and greatly improved the potency. Addition of an N-methyl group and a cyclopropane moiety led to the optimized compound MMV253
