Paper
Novel 6-hydroxy-3-morpholinones as cornea permeable calpain inhibitors.
Published Dec 1, 2003 · Masayuki Nakamura, Hiroyuki Miyashita, Masazumi Yamaguchi
Bioorganic & medicinal chemistry
Q2 SJR score
19
Citations
1
Influential Citations
Abstract
Abstract hidden due to publisher request; this does not indicate any issues with the research. Click the full text link above to read the abstract and view the original source.
Study Snapshot
6-hydroxy-3-morpholinones show promising potential as cornea permeable calpain inhibitors with improved stability and better corneal permeability compared to aldehyde inhibitors 24 and 24a.
PopulationOlder adults (50-71 years)
Sample size24
MethodsObservational
OutcomesBody Mass Index projections
ResultsSocial networks mitigate obesity in older groups.
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References
Exploration of cornea permeable calpain inhibitors as anticataract agents.
Cyclic hemiacetal 4 shows potent inhibitory activities, high cornea permeability, and excellent efficacy in the rat lens culture cataract model.
2003·26citations·Masayuki Nakamura et al.·Bioorganic & medicinal chemistry
Bioorganic & medicinal chemistry
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.
N-(4-fluorophenylsulfonyl)-l-valyl-l-leucinal (SJA6017) is a potent calpain inhibitor with a relatively safe profile, potentially benefiting cancer treatment.
2003·54citations·J. Inoue et al.·Journal of medicinal chemistry
Journal of medicinal chemistry
The calpain family and human disease.
The calpain family, which now includes 14 members, is linked to various diseases, including neurological disorders, Alzheimer's disease, limb-girdle muscular dystrophy, type 2 diabetes, and gastric cancer.
2001·480citations·Yuanhui Huang et al.·Trends in molecular medicine
Trends in molecular medicine
Proteolysis by m-calpain enhances in vitro light scattering by crystallins from human and bovine lenses
Proteolysis by m-calpain enhances heat-induced light scattering in human and bovine lens crystallins, potentially contributing to lens insolubilization during cataract formation in species like man and cows.
2001·34citations·M. Shih et al.·Current Eye Research
Current Eye Research
A survey of calpain inhibitors.
Calpain inhibitors, both natural and synthetic, show promise as therapeutic targets for various diseases, with potential for future development of cell permeable nonpeptide inhibitors.
2000·136citations·I. Donkor·Current medicinal chemistry
Current medicinal chemistry
Citations
Synthesis, antiproliferative evaluation and in silico studies of a novel steroidal spiro morpholinone
The novel steroidal spiro morpholinone derivative shows potent antiproliferative activity against estrogen-dependent and independent solid tumor cell lines, with potential for use in aromatase inhibitor-based cancer treatments.
2023·2citations·Luis A. Cobos-Ontiveros et al.·Steroids
Steroids
Synthesis and transformations of polysubstituted diastereomeric 5-oxomorpholin-2-carboxylic acids
Polysubstituted diastereomeric 5-oxomorpholin-2-carboxylic acids can be synthesized and transformed into peptide bonds, with various configurations and preferred conformations determined by 1H NMR and X-ray analysis.
2014·9citations·N. Burdzhiev et al.·Comptes Rendus Chimie
Comptes Rendus Chimie
Analysis of the structure of calpain-10 and its interaction with the protease inhibitor SNJ-1715
The 3D structure of calpain-10 suggests its active site is conserved among family members, with similarities to -calpain, and its binding to the protease inhibitor SNJ-1715 provides insights into its inhibition mechanism.
2013·4citations·R. C. Silva et al.·Computers in biology and medicine
Computers in biology and medicine
Synthesis of 2-hydroxy-1,4-oxazin-3-ones through ring transformation of 3-hydroxy-4-(1,2-dihydroxyethyl)-β-lactams and a study of their reactivity.
Sodium periodate-mediated oxidation of 3-hydroxy-4-(1,2-dihydroxyethyl)--lactams leads to the exclusive formation of new 2-hydroxy-1,4-oxazin-3-ones, offering potential as building blocks for various oxazin-3-ones
2013·16citations·Karen Mollet et al.·Chemistry
Chemistry
Pyrazine alkaloids via dimerization of amino acid-derived α-amino aldehydes: biomimetic synthesis of 2,5-diisopropylpyrazine, 2,5-bis(3-indolylmethyl)pyrazine and actinopolymorphol C.
Dimerization of amino acid-derived -amino aldehydes provides a short, biomimetic synthesis of various 2,5-disubstituted pyrazine natural products, demonstrating the viability of an alternative biosynthetic route.
2012·17citations·Sandhya Badrinarayanan et al.·Organic & biomolecular chemistry
Organic & biomolecular chemistry
Calpain inhibitors: a survey of compounds reported in the patent and scientific literature
Calpain inhibitors show promise in animal models of calpain-related diseases, but progress into clinical trials is hindered by lack of isoform selectivity and general reactivity.
2011·81citations·I. Donkor·Expert Opinion on Therapeutic Patents
Expert Opinion on Therapeutic Patents
Total syntheses of tubulysins.
Tubulysins D, U, and V are potent tubulin polymerization inhibitors, and their total syntheses were achieved using various methodologies and their biological activities are reported.
2010·58citations·Taku Shibue et al.·Chemistry
Chemistry
Synthesis of 2,2,6,6-tetrafluoro-4-phenylmethylmorpholin-3-ones: A simple approach from fluorinated triethylene glycol
A new single-step method for synthesizing 2,2,6,6-tetrafluoro-4-phenylmethylmorpholin-3-ones using fluorinated triethylene glycol and benzylamine has been developed.
2009·4citations·Zhuo Zeng et al.·Journal of Fluorine Chemistry
Journal of Fluorine Chemistry