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Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
McCombie, Stuart W; Tagat, Jayaram R; Vice, Susan F; Lin, Sue-Ing; Steensma, Ruo; Palani, Anandan; Neustadt, Bernard R; Baroudy, Bahige M; Strizki, Julie M; Endres, Michael; Cox, Kathleen; Dan, Niya; Chou, Chuan-Chu.
Afiliação
  • McCombie SW; Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-2B-2800, Kenilworth, NJ 07033, USA.
Bioorg Med Chem Lett ; 13(3): 567-71, 2003 Feb 10.
Article em En | MEDLINE | ID: mdl-12565973
ABSTRACT
The unsymmetrical nicotinamide-N-oxide moiety in compound 1 was replaced with symmetrical isonicotinamides as well as 4,6-dimethyl pyrimidine-5-carboxamides. Compound 16 from the latter set reduced the number of rotamers, improved potency of inhibiting UIV entry, slightly diminished the affinity for the muscarine receptors and showed very good oral absorption.
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Base de dados: MEDLINE Assunto principal: Piperazinas / HIV-1 / Fármacos Anti-HIV / Antagonistas dos Receptores CCR5 Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2003 Tipo de documento: Article
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PubMed Links

Base de dados: MEDLINE Assunto principal: Piperazinas / HIV-1 / Fármacos Anti-HIV / Antagonistas dos Receptores CCR5 Tipo de estudo: Prognostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2003 Tipo de documento: Article