3区 · 医学
Article
作者: Haarhoff, Zuzana ; Donoso, Maria ; Yin, Zhiwei ; Eastman, Kyle ; Zhang, Zhongxing ; Wang, Tao ; Parker, Dawn ; Meanwell, Nicholas A. ; Roberts, Susan B. ; Yeung, Kap-Sun ; Soars, Matthew G. ; Fang, Hua ; Zvyaga, Tatyana ; Kadow, John F. ; Liu, Mengping ; Rigat, Karen ; Zhu, Juliang ; Hanumegowda, Umesh ; Tuttle, Maria ; Grant-Young, Katharine A. ; Wang, Ying-Kai ; Parcella, Kyle ; Zhuo, Xiaoliang ; Lemm, Julie ; Mosure, Kathy
Iterative structure-activity analyses in a class of highly functionalized furo[2,3-b]pyridines led to the identification of the second generation pan-genotypic hepatitis C virus NS5B polymerase primer grip inhibitor BMT-052 (14), a potential clinical candidate. The key challenge of poor metabolic stability was overcome by strategic incorporation of deuterium at potential metabolic soft spots. The preclinical profile and status of BMT-052 (14) is described.