Using the morpholine core of <b>MK-8718</b> as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV protease inhibitor containing this core showed an 80-fold increase in enzyme binding affinity and a 20-fold increase in antiviral activity relative to <b>MK-8718</b>.

Design and synthesis of bicyclic piperazine sulfonamides leading to highly potent HIV protease inhibitors

254th National Meeting (2017)

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