期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 21, 页码 3339-3342出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm015526o
关键词
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Structure-activity studies on piperidino-piperidine 3 led to the discovery of SCH 351125 (1), a selective CCR5 antagonist with potent activity against RANTES binding (K-i = 2 nM), which possesses subnanomolar activity in blocking viral entry and has excellent antiviral potency versus a panel of primary HIV-1 viral isolates. Compound 1, which has good oral bioavailability in rats, dogs, and monkeys, is proposed as a potential therapeutic agent for the treatment of HIV-1 and has entered human clinical trials.
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