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Phenyl bioisosteres in medicinal chemistry: discovery of novel γ-secretase modulators as a potential treatment for Alzheimer's disease.
Ratni, H; Baumann, K; Bellotti, P; Cook, X A; Green, L G; Luebbers, T; Reutlinger, M; Stepan, A F; Vifian, W.
Afiliación
  • Ratni H; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Baumann K; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Bellotti P; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Cook XA; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Green LG; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Luebbers T; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Reutlinger M; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Stepan AF; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
  • Vifian W; pRED, Pharma Research & Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. Grenzacherstrasse 124 4070 Basel Switzerland hasane.ratni@roche.com (+41) 61 688 2748.
RSC Med Chem ; 12(5): 758-766, 2021 May 26.
Article en En | MEDLINE | ID: mdl-34124674
Phenyl rings are one of the most prevalent structural moieties in active pharmaceutical ingredients, even if they often contribute to poor physico-chemical properties. Herein, we propose the use of a bridged piperidine (BP) moiety as a phenyl bioisostere, which could also be seen as a superior phenyl alternative as it led to strongly improved drug like properties, in terms of solubility and lipophilicity. Additionally, this BP moiety compares favorably to the recently reported saturated phenyl bioisosteres. We applied this concept to our γ-secretase modulator (GSM) project for the potential treatment of Alzheimer's disease delivering clinical candidates.

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: RSC Med Chem Año: 2021 Tipo del documento: Article Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: RSC Med Chem Año: 2021 Tipo del documento: Article Pais de publicación: Reino Unido