Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.

Simon, Petr; Baszczynski, Ondrej; Saman, David; Stepan, George; Hu, Eric; Lansdon, Eric B; Jansa, Petr; Janeba, Zlatko

Simon, Petr; Baszczynski, Ondrej; Saman, David; Stepan, George; Hu, Eric; Lansdon, Eric B; Jansa, Petr; Janeba, Zlatko.

Afiliação

Simon P; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, Prague-6 CZ-16610, Czech Republic.
Baszczynski O; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, Prague-6 CZ-16610, Czech Republic.
Saman D; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, Prague-6 CZ-16610, Czech Republic.
Stepan G; Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Hu E; Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Lansdon EB; Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Jansa P; Gilead Sciences Inc., 333 Lakeside Drive, Foster City, CA 94404, USA.
Janeba Z; Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo nám. 2, Prague-6 CZ-16610, Czech Republic. Electronic address: janeba@uochb.cas.cz.

Eur J Med Chem ; 122: 185-195, 2016 Oct 21.

Article em En | MEDLINE | ID: mdl-27371922

Assuntos

Desenho de Fármacos; Transcriptase Reversa do HIV/antagonistas & inibidores; HIV-1/enzimologia; Pirimidinas/química; Pirimidinas/farmacologia; Inibidores da Transcriptase Reversa/química; Inibidores da Transcriptase Reversa/farmacologia; Transcriptase Reversa do HIV/química; Transcriptase Reversa do HIV/metabolismo; HIV-1/efeitos dos fármacos; Simulação de Acoplamento Molecular; Conformação Proteica; Pirimidinas/metabolismo; Inibidores da Transcriptase Reversa/metabolismo

Palavras-chave

Diarylpyrimidine (DAPY); Etravirine; Human immunodeficiency virus (HIV); NNRTIs; Non-nucleoside reverse transcriptase inhibitors; Rilpivirine

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Desenho de Fármacos / HIV-1 / Inibidores da Transcriptase Reversa / Transcriptase Reversa do HIV Idioma: En Ano de publicação: 2016 Tipo de documento: Article

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