368-22-9Relevant academic research and scientific papers
Synthesis and anti-HIV-1 activity evaluation for novel 3a,6a-dihydro-1H-pyrrolo[3,4-c]pyrazole-4,6-dione derivatives
Liu, Guan-Nan,Luo, Rong-Hua,Zhou, Yu,Zhang, Xing-Jie,Li, Jian,Yang, Liu-Meng,Zheng, Yong-Tang,Liu, Hong
, (2016)
The search for new molecular constructs that resemble the critical two-metal binding pharmacophore and the halo-substituted phenyl functionality required for HIV-1 integrase (IN) inhibition represents a vibrant area of research within drug discovery. As reported herein, we have modified our recently disclosed 1-[2-(4-fluorophenyl)ethyl]-pyrrole-2,5-dione scaffolds to design 35 novel compounds with improved biological activities against HIV-1. These new compounds show single-digit micromolar antiviral potencies against HIV-1 and low toxicity. Among of them, compound 9g and 15i had potent anti-HIV-1 activities (EC50 50 /EC50 > 100). These two compounds have potential as lead compounds for further optimization into clinical anti-HIV-1 agents.
