Stepwise Design of Î³-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.

Rodríguez Sarmiento, Rosa María; Bissantz, Caterina; Bylund, Johan; Limberg, Anja; Neidhart, Werner; Jakob-Roetne, Roland; Wang, Lisha; Baumann, Karlheinz

Rodríguez Sarmiento, Rosa María; Bissantz, Caterina; Bylund, Johan; Limberg, Anja; Neidhart, Werner; Jakob-Roetne, Roland; Wang, Lisha; Baumann, Karlheinz.

Afiliação

Rodríguez Sarmiento RM; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Bissantz C; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Bylund J; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Limberg A; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Neidhart W; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Jakob-Roetne R; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Wang L; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.
Baumann K; Pharmaceutical Research and Early Development, F. Hoffmann-La Roche AG, Roche Innovation Center Basel, Grenzacherstrasse 124, 4070 Basel, Switzerland.

J Med Chem ; 63(15): 8534-8553, 2020 08 13.

Article em En | MEDLINE | ID: mdl-32706964

Assuntos

Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores; Secretases da Proteína Precursora do Amiloide/metabolismo; Desenho de Fármacos; Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacologia; Peptídeos beta-Amiloides/metabolismo; Animais; Linhagem Celular; Inibidores Enzimáticos/farmacocinética; Humanos; Camundongos Transgênicos; Modelos Moleculares; Neurônios/efeitos dos fármacos; Neurônios/metabolismo

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Inibidores Enzimáticos / Secretases da Proteína Precursora do Amiloide Limite: Animals / Humans Idioma: En Ano de publicação: 2020 Tipo de documento: Article

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