Abstract
Herein we describe the drug design steps developed to increase the radical scavenging and β-amyloid aggregation inhibitory activities of a previously described series of benzylidenephenylpyrrolizinones. Among the newly synthesized derivatives, some benzylphenylpyrrolizinones exhibited interesting results in regard to those activities. Initial druggability parameters were measured, and suggest these compounds as a suitable starting point for potential alternatives in treating Alzheimer's disease.
Keywords:
Alzheimer′s disease; MTDL; antioxidants; pyrrolizinones; β-amyloid.
© 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-2 Receptor Antagonists / chemical synthesis
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Adrenergic alpha-2 Receptor Antagonists / chemistry
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Adrenergic alpha-2 Receptor Antagonists / pharmacology*
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Alzheimer Disease / drug therapy*
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Amyloid beta-Peptides / antagonists & inhibitors*
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Dose-Response Relationship, Drug
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Drug Design
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Free Radical Scavengers / chemical synthesis
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Free Radical Scavengers / chemistry
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Free Radical Scavengers / pharmacology*
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Humans
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Models, Molecular
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Molecular Structure
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Protein Aggregates / drug effects
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Pyrrolizidine Alkaloids / chemical synthesis
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Pyrrolizidine Alkaloids / chemistry
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Pyrrolizidine Alkaloids / pharmacology*
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Structure-Activity Relationship
Substances
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Adrenergic alpha-2 Receptor Antagonists
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Amyloid beta-Peptides
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Free Radical Scavengers
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Protein Aggregates
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Pyrrolizidine Alkaloids