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.
J Med Chem
; 44(21): 3339-42, 2001 Oct 11.
Article
em En
| MEDLINE
| ID: mdl-11585437
ABSTRACT
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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Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Piperidinas
/
Piridinas
/
Fármacos Anti-HIV
/
Óxidos N-Cíclicos
/
Antagonistas dos Receptores CCR5
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article