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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-21 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00386 Christopher J. Bungard 1 , Peter D. Williams 1 , Jurgen Schulz 1 , Catherine M. Wiscount 1 , M. Katharine Holloway 1 , H. Marie Loughran 1 , Jesse J. Manikowski 1 , Hua-Poo Su 1 , David J. Bennett 1 , Lehua Chang 2 , Xin-Jie Chu 2 , Alejandro Crespo 2 , Michael P. Dwyer 2 , Kartik Keertikar 2 , Gregori J. Morriello 2 , Andrew W. Stamford 2 , Sherman T. Waddell 2 , Bin Zhong 3 , Bin Hu 3 , Tao Ji 3 , Tracy L. Diamond 1 , Carolyn Bahnck-Teets 1 , Steven S. Carroll 1 , John F. Fay 1 , Xu Min 1 , William Morris 2 , Jeanine E. Ballard 1 , Michael D. Miller 1 , John A. McCauley 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-11-21 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00386 Christopher J. Bungard 1 , Peter D. Williams 1 , Jurgen Schulz 1 , Catherine M. Wiscount 1 , M. Katharine Holloway 1 , H. Marie Loughran 1 , Jesse J. Manikowski 1 , Hua-Poo Su 1 , David J. Bennett 1 , Lehua Chang 2 , Xin-Jie Chu 2 , Alejandro Crespo 2 , Michael P. Dwyer 2 , Kartik Keertikar 2 , Gregori J. Morriello 2 , Andrew W. Stamford 2 , Sherman T. Waddell 2 , Bin Zhong 3 , Bin Hu 3 , Tao Ji 3 , Tracy L. Diamond 1 , Carolyn Bahnck-Teets 1 , Steven S. Carroll 1 , John F. Fay 1 , Xu Min 1 , William Morris 2 , Jeanine E. Ballard 1 , Michael D. Miller 1 , John A. McCauley 1
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Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core showed an 60-fold increase in enzyme binding affinity and a 10-fold increase in antiviral activity relative to MK-8718.
中文翻译：
设计和合成导致高强度HIV-1蛋白酶抑制剂的哌嗪磺酰胺核心。
以MK-8718和PL-100的HIV-1蛋白酶结合模式为灵感，设计并合成了一种新型的天冬氨酸结合双环哌嗪磺酰胺核心。相对于MK-8718，所得的含有该核心的HIV-1蛋白酶抑制剂显示出酶结合亲和力增加了60倍，抗病毒活性增加了10倍。
更新日期：2017-11-21
中文翻译：
设计和合成导致高强度HIV-1蛋白酶抑制剂的哌嗪磺酰胺核心。
以MK-8718和PL-100的HIV-1蛋白酶结合模式为灵感，设计并合成了一种新型的天冬氨酸结合双环哌嗪磺酰胺核心。相对于MK-8718，所得的含有该核心的HIV-1蛋白酶抑制剂显示出酶结合亲和力增加了60倍，抗病毒活性增加了10倍。
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