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Proteins, Expression, Isolation and Analysis | … Acknowledgments. We thank Dr. Xinbo Jiang from GenScript USA Inc. for the tests of inhibitory activity of human ERG channels, Prof. Zhengqing Zhang from Beijing Institute of Toxicology and Pharmacology for the determination of pharmacokinetics … | Get A Quote |
A series of novel 1,4-disubstituted piperidine/piperazine derivatives were designed, synthesized and evaluated for their in vitro activities against HIV-1 Bal (R5) infection in CEMX174 5.25M7 cells. A majority of these compounds showed potent anti-HIV-1 activities with IC(50) at nanomolar levels. N-(4-Fluoro-benzyl)piperazine analog B07 hydrochloride exhibited potency against HIV-1 activity similar to that of TAK-220 hydrochloride, but it had much better water solubility (25 mg/ml in phosphate sodium buffer at 25 °C) and oral bioavailability (56%) than TAK-220 hydrochloride (a solubility of 2 mg/ml and oral bioavailability of 1.4%). These results suggest that B07 hydrochloride may serve as a better lead ... More