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In this work, stereoselective fluorination is investigated as a strategy for enhancing the potency of WEHI\u2010601 through conformational bias. Consistent with prediction, a fluorostatine\u2010containing analogue of WEHI\u2010601 is found to deliver stronger antimalarial activity than the lead compound, attributable to conformational preorganisation of the F\uf8ffC\uf8ffC\uf8feO segment within the peptidomimetic backbone. 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