| Design, synthesis and docking studies of Hydroxyethylamine and Hydroxyethylsulfide BACE-1 inhibitors. | |
| | |
MedLine Citation:
|
PMID: 19149679 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Both stereoisomer of hydroxyethylamine (HEA) and hydroxyethylsulfide (HES) transition-state isostere inhibitors of BACE-1 were synthesized. The syn-HEA epimer resulted always more active than the anti stereoisomer independently from the P(1) and the P(1)' substituents. On the contrary, the anti epimer of the HES isostere resulted more active than the syn stereoisomer. The change of stereopreference was studied by molecular modelling. |
| | |
Authors:
|
Luca Rizzi; Nadia Vaiana; Francesca Sagui; Eva Genesio; Elena Pilli; Valentina Porcari; Sergio Romeo |
Related Documents
:
|
16122209 - Suboccipital burr holes and craniectomies. 7615499 - Cytochrome b-245 of the neutrophil superoxide-generating system contains two nonidentic... 21739859 - Use of domperidone to enhance lactation: what is the evidence? 14767259 - Pedometer measures of free-living physical activity: comparison of 13 models. 22840619 - Star-crossed? the association of the 5-httlpr s allele with season of birth in a health... 1118439 - Resuscitation of the newborn. 8528189 - Distribution of fibronectin in foetal tissues. 22925469 - A systematic review of risk factors during first year of life for early childhood caries. 8708929 - Fetal monitoring by combined ctg and fba. |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Protein and peptide letters Volume: 16 ISSN: 0929-8665 ISO Abbreviation: Protein Pept. Lett. Publication Date: 2009 |
Date Detail:
|
Created Date: 2009-01-19 Completed Date: 2009-03-05 Revised Date: 2009-11-19 |
Medline Journal Info:
|
Nlm Unique ID: 9441434 Medline TA: Protein Pept Lett Country: Netherlands |
Other Details:
|
Languages: eng Pagination: 86-90 Citation Subset: IM |
Affiliation:
|
Institute of Medicinal Chemistry "Pietro Pratesi", School of Pharmacy, University of Milan, Via Mangiagalli 25, 20133, Milan, Italy. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Amyloid Precursor Protein Secretases
/
antagonists & inhibitors* Aspartic Acid Endopeptidases / antagonists & inhibitors* Biomimetic Materials Drug Design Ethylamines / chemical synthesis*, chemistry Protease Inhibitors / chemical synthesis*, chemistry* Stereoisomerism Structure-Activity Relationship Sulfhydryl Compounds / chemical synthesis*, chemistry |
| Chemical | |
Reg. No./Substance:
|
0/Ethylamines; 0/Protease Inhibitors; 0/Sulfhydryl Compounds; EC 3.4.-/Amyloid Precursor Protein Secretases; EC 3.4.23.-/Aspartic Acid Endopeptidases; EC 3.4.23.46/BACE1 protein, human |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Pomegranin, an antifungal peptide from pomegranate peels.
Next Document: Proteinase K-resistant aggregates of recombinant prion protein PrP-(23-98) are toxic to cultured cel...