Design, synthesis, and in silico studies of tetrahydropyrimidine analogs as urease enzyme inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200158
Abstract: The urease enzyme, a metalloenzyme having Ni2+ ions, is recognized in some bacteria, fungi, and plants. Particularly, it is vital to the progress of infections induced by pathogenic microbes, such as Proteus mirabilis and Helicobacter… read more here.
Keywords: urease enzyme; silico studies; activity; inhibitory activity ... See more keywords
N‐Substituted piperidine‐3‐carbohydrazide‐hydrazones against Alzheimer's disease: Synthesis and evaluation of cholinesterase, beta‐amyloid inhibitory activity, and antioxidant capacity
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200519
Abstract: A series of piperidine‐3‐carbohydrazide‐hydrazones bearing phenylethyl, phenylpropyl, and phenylbutyl substituents on piperidine nitrogen were designed and synthesized as cholinesterase (ChE) inhibitors. The title compounds were screened for acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) inhibitory activities and antioxidant… read more here.
Keywords: piperidine carbohydrazide; alzheimer disease; inhibitory activity; inhibitory ... See more keywords
Bacterially Secretable Single‐Chain Tandem Macrocyclic Peptides for High Affinity and Inhibitory Activity
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DOI: 10.1002/cbic.202200599
Abstract: The inhibition of protein‐protein interactions (PPIs) is an effective approach for therapy. Owing to their large binding surface areas to target proteins, macrocyclic peptides are suitable molecules for PPI inhibition. In this study, we developed… read more here.
Keywords: chain tandem; macrocyclic peptides; inhibitory activity; single chain ... See more keywords
7‐Amidocoumarins as Multitarget Agents against Neurodegenerative Diseases: Substitution Pattern Modulation
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DOI: 10.1002/cmdc.202000454
Abstract: This study explores the potential of 7‐amidocoumarins as multitarget agents against Parkinson's and Alzheimer's diseases, by modulating the substitution patterns within the scaffold. Sixteen compounds were synthesized via 7‐amino‐4‐methylcoumarin acylation, and in vitro evaluation of the… read more here.
Keywords: substitution pattern; amidocoumarins multitarget; multitarget agents; substitution ... See more keywords
Synthesis of a β‐d‐Psicofuranosyl Sulfone and Inhibitory‐Activity Evaluation Against N‐Acetylglucosaminyltransferase I
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Organic Chemistry"
DOI: 10.1002/ejoc.201701102
Abstract: Alkyl or aryl 3-acetamido-3-deoxy-2-thio-β-d-psicofuranosides bearing a phosphate group at C-1, which were originally designed as potential GnT-I inhibitors (GnT = N-acetylglucosaminyltransferase) by computational methods, were found to be unstable. Therefore their structure was slightly modified… read more here.
Keywords: inhibitor; psicofuranosyl; psicofuranosyl sulfone; inhibitory activity ... See more keywords
Evaluation of xanthine oxidase inhibitory activity of flavonoids by an on-line capillary electrophoresis-based immobilized enzyme microreactor.
Sign Up to like & getrecommendations! Published in 2020 at "Electrophoresis"
DOI: 10.1002/elps.202000083
Abstract: Xanthine oxidase (XOD) is a key enzyme in the human body to produce uric acid, and its inhibitor can be used for the treatment of hyperuricemia and gout. In this study, an on-line capillary electrophoresis… read more here.
Keywords: xod; line; enzyme; inhibitory activity ... See more keywords
Investigating inhibitory activity of novel synthetic sericin peptide on α-D-glucosidase: kinetics and interaction mechanism study using a docking simulation.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of the science of food and agriculture"
DOI: 10.1002/jsfa.8620
Abstract: BACKGROUND We synthesised a novel sericin peptide (SP-GI) with α-d-glucosidase inhibitory activity, which has a sequence of SEDSSEVDIDLGN. The kinetics of its peptide-induced inhibition on α-d-glucosidase activity and its interaction mechanism merging with molecular docking… read more here.
Keywords: mechanism; sericin peptide; interaction; glucosidase ... See more keywords
Mechanism study of multimode ultrasound pretreatment on the enzymolysis of wheat gluten.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of the science of food and agriculture"
DOI: 10.1002/jsfa.8624
Abstract: BACKGROUND Ultrasound pretreatment could improve the angiotensin-I converting enzyme (ACE) inhibitory activity of hydrolysates of wheat gluten (WG). The working mode of ultrasound has an important effect on the enzymatic hydrolysis of protein. RESULTS The… read more here.
Keywords: enzymolysis; ace inhibitory; wheat gluten; ultrasound pretreatment ... See more keywords
Evaluation inhibitory activity of catechins on trypsin by capillary electrophoresis-based immobilized enzyme microreactor with chromogenic substrate.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of separation science"
DOI: 10.1002/jssc.202000132
Abstract: In this study, a capillary electrophoresis-based online immobilized enzyme microreactor was developed for evaluating the inhibitory activity of green tea catechins and tea polyphenol extracts on trypsin. The immobilized trypsin activity and other kinetic parameters… read more here.
Keywords: inhibitory activity; activity; immobilized enzyme; tea ... See more keywords
Antibacterial and β‐Lactamase Inhibitory Activity of Monocyclic β‐Lactams
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DOI: 10.1002/med.21443
Abstract: Due to the widespread emergence of resistant bacterial strains, an urgent need for the development of new antibacterial agents with novel modes of action has emerged. The discovery of naturally occurring monocyclic β‐lactams in the… read more here.
Keywords: lactamase inhibitory; inhibitory activity; monocyclic lactams; antibacterial lactamase ... See more keywords
Rational Design and Identification of Novel Thiosemicarbazide Derivatives as Laccase Inhibitors.
Sign Up to like & getrecommendations! Published in 2023 at "Pest management science"
DOI: 10.1002/ps.7562
Abstract: BACKGROUND Laccase is a key enzyme in the fungal 1,8-dihydroxynaphthalene(DHN) melanin biosynthesis pathway, which is a potential target for the control of pathogenic fungi. In our previous work, a2 was found with higher inhibition activity… read more here.
Keywords: rational design; laccase; activity laccase; inhibitory activity ... See more keywords