Journal of medicinal chemistry, 2001-10, Vol.44 (21), p.3339-3342
2001
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Details
- Autor(en) / Beteiligte
- Titel
- Discovery of 4-[(Z)-(4-Bromophenyl)- (ethoxyimino)methyl]-1‘-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4‘-methyl-1,4‘- bipiperidine N-Oxide (SCH 351125): An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection
- Ist Teil von
- Journal of medicinal chemistry, 2001-10, Vol.44 (21), p.3339-3342
- Ort / Verlag
- Washington, DC: American Chemical Society
- Erscheinungsjahr
- 2001
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm015526oTitel-ID: cdi_proquest_miscellaneous_71220090
- Format
- –
- Schlagworte
- Administration, Oral, Animals, Anti-HIV Agents - chemical synthesis, Anti-HIV Agents - chemistry, Anti-HIV Agents - pharmacokinetics, Anti-HIV Agents - pharmacology, Antibiotics. Antiinfectious agents. Antiparasitic agents, Antiviral agents, Biological and medical sciences, Biological Availability, CCR5 Receptor Antagonists, Cell Line, Cyclic N-Oxides - chemical synthesis, Cyclic N-Oxides - chemistry, Cyclic N-Oxides - pharmacokinetics, Cyclic N-Oxides - pharmacology, Dogs, Drug Evaluation, Preclinical, HIV-1 - drug effects, Humans, In Vitro Techniques, Leukocytes, Mononuclear - virology, Macaca fascicularis, Medical sciences, Pharmacology. Drug treatments, Piperazines - chemical synthesis, Piperazines - chemistry, Piperazines - pharmacokinetics, Piperazines - pharmacology, Piperidines, Pyridines - chemical synthesis, Pyridines - chemistry, Pyridines - pharmacokinetics, Pyridines - pharmacology, Rats, Structure-Activity Relationship