Synthesis, Structure-Activity Relationships and Brain Uptake of a Novel Series of Benzopyran Inhibitors of Insulin-Regulated Aminopeptidase

Peptide inhibitors of insulin-regulated aminopeptidase (IRAP) enhance fear avoidance and spatial memory and accelerate spatial learning in a number of memory paradigms. Using a virtual screening approach, a series of benzopyran compounds was identified that inhibited the catalytic activity of IRAP,...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 57; no. 4; pp. 1368 - 1377
Main Authors:	Mountford, Simon J., Albiston, Anthony L., Charman, William N., Ng, Leelee, Holien, Jessica K., Parker, Michael W., Nicolazzo, Joseph A., Thompson, Philip E., Chai, Siew Yeen
Format:	Journal Article
Language:	English
Published:	WASHINGTON Amer Chemical Soc 27.02.2014
Subjects:	Aminopeptidases - antagonists & inhibitors Animals Benzopyrans - chemical synthesis Benzopyrans - chemistry Benzopyrans - pharmacokinetics Benzopyrans - pharmacology Brain - metabolism Cell Line Chemistry, Medicinal Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Insulin - pharmacology Life Sciences & Biomedicine Magnetic Resonance Spectroscopy Pharmacology & Pharmacy Rats Science & Technology Spectrometry, Mass, Electrospray Ionization Structure-Activity Relationship WATER MAZE POTENT (IRAP)/AT RECEPTOR LIGANDS LVV-HEMORPHIN-7 ANGIOTENSIN-IV ATTENUATION RATS SPATIAL MEMORY DEFICITS PASSIVE-AVOIDANCE
ISSN:	0022-2623, 1520-4804, 1520-4804
Online Access:	Get more information
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