1202645-23-5Relevant articles and documents
Inhibitors of HIV-1 attachment: The discovery and structure-activity relationships of tetrahydroisoquinolines as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore
Swidorski, Jacob J.,Liu, Zheng,Yin, Zhiwei,Wang, Tao,Carini, David J.,Rahematpura, Sandhya,Zheng, Ming,Johnson, Kim,Zhang, Sharon,Lin, Pin-Fang,Parker, Dawn D.,Li, Wenying,Meanwell, Nicholas A.,Hamann, Lawrence G.,Regueiro-Ren, Alicia
, p. 160 - 167 (2015/12/18)
6,6-Fused ring systems including tetrahydroisoquinolines and tetrahydropyrido[3,4-d]pyrimidines have been explored as possible replacements for the piperazine benzamide portion of the HIV-1 attachment inhibitor BMS-663068. In initial studies, the tetrahydroisoquinoline compounds demonstrate sub-nanomolar activity in a HIV-1 pseudotype viral infection assay used as the initial screen for inhibitory activity. Analysis of SARs and approaches to optimization for an improved drug-like profile are examined herein.