Synthesis and Glycosidase Inhibition Studies of 5-Methyl-Substituted Tetrahydroxyindolizidines and -pyrrolizidines Related to Natural Hyacinthacines B

2013 ◽  
Vol 2013 (19) ◽  
pp. 4047-4056 ◽  
Author(s):  
Daniele Martella ◽  
Francesca Cardona ◽  
Camilla Parmeggiani ◽  
Francisco Franco ◽  
Juan A. Tamayo ◽  
...  
Keyword(s):  
Inhibition Studies ◽  
Glycosidase Inhibition

Design, synthesis and glycosidase inhibition studies of novel triazole fused iminocyclitol-δ-lactams

2019 ◽  
Vol 17 (5) ◽  
pp. 1130-1140 ◽  
Author(s):  
Venkatesan Santhanam ◽  
Pradeep Pant ◽  
B. Jayaram ◽  
Namakkal G. Ramesh
Keyword(s):  
Design Synthesis ◽  
Key Steps ◽  
Inhibition Studies ◽  
Glycosidase Inhibition

Synthesis of novel triazole fused iminocyclitol-δ-lactams, from tri-O-benzyl-d-glucal, involving intermolecular [3 + 2]cycloaddition and intramolecular lactamisation reactions as key steps is described.

A New Access to Polyhydroxy Piperidines of the Azasugar Class: Synthesis and Glycosidase Inhibition Studies.

ChemInform ◽  
2004 ◽  
Vol 35 (8) ◽  
Author(s):  
Ganesh Pandey ◽  
Manmohan Kapur ◽  
M. Islam Khan ◽  
Sushama M. Gaikwad
Keyword(s):  
Inhibition Studies ◽  
Glycosidase Inhibition

A new access to polyhydroxy piperidines of the azasugar class: synthesis and glycosidase inhibition studies

2003 ◽  
Vol 1 (19) ◽  
pp. 3321 ◽  
Author(s):  
Ganesh Pandey ◽  
Manmohan Kapur ◽  
M. Islam Khan ◽  
Sushama M. Gaikwad
Keyword(s):  
Inhibition Studies ◽  
Glycosidase Inhibition

Difference of [Ca2+]i Movements in Platelets Stimulated by Thrombin and TRAP: the Involvement of αIIbβ3-Mediated TXA2 Synthesis

1998 ◽  
Vol 79 (06) ◽  
pp. 1184-1190 ◽  
Author(s):  
Yoshiaki Tomiyama ◽  
Shigenori Honda ◽  
Kayoko Senzaki ◽  
Akito Tanaka ◽  
Mitsuru Okubo ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Fibrinogen Binding ◽  
Adp Release ◽  
The Difference ◽  
Txa2 Receptor Antagonist ◽  
High Level ◽  
Inhibition Studies ◽  
Peak Increase ◽  
Second Peak ◽  
Assay Conditions

SummaryThis study investigated the difference of [Ca2+]i movement in platelets in response to thrombin and TRAP. The involvement of αIIbβ3 in this signaling was also studied. Stimulation of platelets with thrombin at 0.03 U/ml caused platelet aggregation and a two-peak increase in [Ca2+]i. The second peak of [Ca2+]i, but not the first peak was abolished by the inhibition of platelet aggregation with αIIbβ3 antagonists or by scavenging endogenous ADP with apyrase. A cyclooxygenase inhibitor, aspirin, and a TXA2 receptor antagonist, BM13505, also abolished the second peak of [Ca2+]i but not the first peak, although these regents did not inhibit aggregation. Under the same assay conditions, measurement of TXB2 demonstrated that αIIbβ3 antagonists and aspirin almost completely inhibited the production of TXB2. In contrast to thrombin-stimulation, TRAP caused only a single peak of [Ca2+]i even in the presence of platelet aggregation, and a high level of [Ca2+]i increase was needed for the induction of platelet aggregation. The inhibition of aggregation with αIIbβ3 antagonists had no effect on [Ca2+]i change and TXB2 production induced by TRAP. Inhibition studies using anti-GPIb antibodies suggested that GPIb may be involved in the thrombin response, but not in the TRAP. Our findings suggest that low dose thrombin causes a different [Ca2+]i response and TXA2 producing signal from TRAP. Endogenous ADP release and fibrinogen binding to αIIbβ3 are responsible for the synthesis of TXA2 which results in the induction of the second peak of [Ca2+]i in low thrombin- but not TRAP-stimulated platelets.

Isolation and Characterization of Plasminogen Activator from Pig Leucocytes

1974 ◽  
Vol 31 (01) ◽  
pp. 072-085 ◽  
Author(s):  
M Kopitar ◽  
M Stegnar ◽  
B Accetto ◽  
D Lebez
Keyword(s):  
Molecular Weight ◽  
Plasminogen Activator ◽  
Gel Electrophoresis ◽  
Gel Filtration ◽  
Ph Optimum ◽  
Isolation And Characterization ◽  
Ph Range ◽  
Inhibition Studies ◽  
Final Purification

SummaryPlasminogen activator was isolated from disrupted pig leucocytes by the aid of DEAE chromatography, gel filtration on Sephadex G-100 and final purification on CM cellulose, or by preparative gel electrophoresis.Isolated plasminogen activator corresponds No. 3 band of the starting sample of leucocyte cells (that is composed from 10 gel electrophoretic bands).pH optimum was found to be in pH range 8.0–8.5 and the highest pH stability is between pH range 5.0–8.0.Inhibition studies of isolated plasminogen activator were performed with EACA, AMCHA, PAMBA and Trasylol, using Anson and Astrup method. By Astrup method 100% inhibition was found with EACA and Trasylol and 30% with AMCHA. PAMBA gave 60% inhibition already at concentration 10–3 M/ml. Molecular weight of plasminogen activator was determined by gel filtration on Sephadex G-100. The value obtained from 4 different samples was found to be 28000–30500.

Mycobacterial DNA GyrB Inhibitors: Ligand Based Pharmacophore Modelling and In Vitro Enzyme Inhibition Studies

2014 ◽  
Vol 14 (17) ◽  
pp. 1990-2005 ◽  
Author(s):  
Shalini Saxena ◽  
Janupally Renuka ◽  
Variam Jeankumar ◽  
Perumal Yogeeswari ◽  
Dharmarajan Sriram
Keyword(s):  
Enzyme Inhibition ◽  
Pharmacophore Modelling ◽  
Inhibition Studies

Synthesis, Characterization and Cholinesterase Inhibition Studies of New Arylidene Aminothiazolylethanone Derivatives

2017 ◽  
Vol 13 (7) ◽  
Author(s):  
Pervaiz A. Channar ◽  
Muhammad S. Shah ◽  
Aamer Saeed ◽  
Shafi U. Khan ◽  
Fayaz A. Larik ◽  
...  
Keyword(s):  
Cholinesterase Inhibition ◽  
Inhibition Studies
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