1272011-41-2Relevant academic research and scientific papers
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents
Li, Ben,Jones, Eric Dale,Zhou, Enkun,Chen, Li,Baylis, Dean Cameron,Yu, Shanghai,Wang, Miao,He, Xing,Coates, Jonathan Alan Victor,Rhodes, David Ian,Pei, Gang,Deadman, John Joseph,Xie, Xin,Ma, Dawei
scheme or table, p. 5334 - 5336 (2010/10/03)
Modification of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists revealed that introducing a fluoro group at the 3-position of the 3-phenyl group to reduce metabolism did not adversely affect the high potency against HIV infection, and that replacing the piperidine ring with a tropane ring could deliver the most potent anti-HIV agents. Stereochemistry of the substituted tropane ring is essential for maintaining the potent anti-HIV activity because only exo-isomers displayed subnanomolar whole cell activity.
