AZD6642, a potent small molecule inhibitor of the 5-lipoxygenase activating protein (FLAP) in the 5-LO pathway, was developed through a fast-follower approach with the objective to optimize a number of key parameters, such as lipophilicity and metabolic stability.Learnings and high-lights from the medicinal chemistry drug discovery program will be covered. In addition, a variety of synthetic routes will be described including the synthesis of three different scaffolds with special attention to the silicon switch strategy.

From idea to candidate drug selection of 5-lipoxygenase activating protein (FLAP) inhibitors including a silicon switch strategy

248th National Meeting (2014)

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