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Piperazine Bioisosteres for Drug Design

More than 100 FDA-approved drugs contain the piperazine moiety. Piperazine-based analogues may advantageously alter important pharmacokinetic properties when grafted onto molecular scaffolds. In 2018, chemists showed that replacing a piperazine ring in the drug Olaparib with the spirodiamine analogue beneficially affected activity and reduced cytotoxicity of the parent compound. Herein we have designed and synthesized a library of piperazine analogues for drug design.

Design

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>100 unique piperazine analogues on a 5-50 g scale from stock.

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