Design and Synthesis of Novel Arylketo-containing P1-P3 Linked Macro-cyclic BACE-1 Inhibitors

Kvarnström, Ingemar (author): Linköpings universitet,Kemi,Tekniska högskolan

(creator_code:org_t)

Bussum, Netherlands : Bentham Open, 2015
2015
English.
In: Open Medicinal Chemistry Journal. - Bussum, Netherlands : Bentham Open. - 1874-1045. ; 9, s. 13-26

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Abstract Subject headings

A series of arylketo-containing P1-P3 linked macrocyclic BACE-1 inhibitors were designed, synthesized, and compared with compounds with a previously known and extensively studied corresponding P2 isophthalamide moiety with the aim to improve on permeability whilst retaining the enzyme- and cell-based activities. Several inhibitors displayed substantial increases in Caco-2 cell-based permeability compared to earlier synthesized inhibitors and notably also with retained activities, showing that this approach might yield BACE-1 inhibitors with improved properties.

By the author/editor: Sandgren, Veroni ...; Belda, Oscar; Kvarnström, Inge ...; Lindberg, Jimmy; Samuelsson, Bert ...; Dahlgren, Anders

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Medicinal Chemis ...

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