Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators

Autor:	Garrett Berlond Minne, Michel Surkyn, Harrie J.M. Gijsen, Francois Paul Bischoff, Nigel Austin, Marc Mercken, Didier Berthelot, Chiara Zavattaro, Ishtiyaque Ahmad, Gregor James Macdonald, Adriana Ingrid Velter, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Sven Franciscus Anna Van Brandt, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Swapan Kumar Samanta, Herman Borghys
Rok vydání:	2019
Předmět:	Indole test Indoles Series (mathematics) Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry In vitro chemistry.chemical_compound Structure-Activity Relationship medicine.anatomical_structure chemistry In vivo Drug Design Drug Discovery medicine Molecular Medicine Potency Imidazole Humans γ secretase Amyloid Precursor Protein Secretases Molecular Biology Nucleus
Zdroj:	Bioorganicmedicinal chemistry letters. 29(14)
ISSN:	1464-3405
Popis:	The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined high in vitro and in vivo potency with an acceptable drug-like profile.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d9f458af2fb6e368fbdd2185f1f9926 https://pubmed.ncbi.nlm.nih.gov/31122869 Zobrazit plný text záznamu Full Text from ScienceDirect