scholarly journals Synthesis and biological evaluation of conformationally restricted adenine bicycloribonucleosides

2015 ◽  
Vol 13 (35) ◽  
pp. 9300-9313 ◽  
Author(s):  
Hubert Hřebabecký ◽  
Eliška Procházková ◽  
Michal Šála ◽  
Pavla Plačková ◽  
Eva Tloušťová ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Conformationally Restricted ◽  
Synthesis And Biological Evaluation

We prepared a novel series of conformationally restricted bicyclonucleosides and nucleotides.

scholarly journals Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues

MedChemComm ◽  
2019 ◽  
Vol 10 (8) ◽  
pp. 1445-1456 ◽  
Author(s):  
Casey J. Maguire ◽  
Graham J. Carlson ◽  
Jacob W. Ford ◽  
Tracy E. Strecker ◽  
Ernest Hamel ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Conformationally Restricted ◽  
Structural Analogues ◽  
Synthesis And Biological Evaluation

Cyclic chalcones and structural analogues evaluated as cytotoxic agents.

Proline–Glutamate Chimeras in Isopeptides. Synthesis and Biological Evaluation of Conformationally Restricted Glutathione Analogues

2003 ◽  
Vol 11 (8) ◽  
pp. 1677-1683 ◽  
Author(s):  
Mario Paglialunga Paradisi ◽  
Adriano Mollica ◽  
Ivana Cacciatore ◽  
Antonio Di Stefano ◽  
Francesco Pinnen ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Conformationally Restricted ◽  
Synthesis And Biological Evaluation

Design, Synthesis, and Biological Evaluation of Conformationally Restricted Rivastigmine Analogues

2004 ◽  
Vol 47 (24) ◽  
pp. 5945-5952 ◽  
Author(s):  
Maria Laura Bolognesi ◽  
Manuela Bartolini ◽  
Andrea Cavalli ◽  
Vincenza Andrisano ◽  
Michela Rosini ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Conformationally Restricted ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of conformationally restricted σ1 receptor ligands with 7,9-diazabicyclo[4.2.2]decane scaffold

2010 ◽  
Vol 8 (24) ◽  
pp. 5525 ◽  
Author(s):  
Sunil K. Sunnam ◽  
Dirk Schepmann ◽  
Elisabeth Rack ◽  
Roland Fröhlich ◽  
Katharina Korpis ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Receptor Ligands ◽  
Conformationally Restricted ◽  
Σ1 Receptor ◽  
Synthesis And Biological Evaluation

Synthesis and biological evaluation of a bicyclo[4.1.0]heptyl analogue of glucose-1-phosphate

2004 ◽  
Vol 82 (9) ◽  
pp. 1361-1364 ◽  
Author(s):  
Veedeeta Dookhun ◽  
Andrew J Bennet
Keyword(s):  
Key Words ◽  
Biological Evaluation ◽  
Dihydrogen Phosphate ◽  
Synthetic Route ◽  
Conformationally Restricted ◽  
Key Words Glucose ◽  
Phosphate Inhibition ◽  
Synthesis And Biological Evaluation ◽  
Potential Substrate

The synthesis of a bicyclo[4.1.0]heptyl analogue of glucose-1-phophate, (1R,2R,3S,4S,5S,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)-bicyclo[4.1.0]heptan-2-yl dihydrogen phosphate (5) is reported. The synthetic route chosen started with methyl α-D-glucopyranoside and was accomplished in 11 steps with an overall yield of 3%. Compound 5 was tested as a potential substrate of UTP:α-D-glucose-1-phosphate uridylyltransferase, the enzyme that converts glucose-1-phosphate into UDP-glucose. However, the conformationally restricted glucose-1-phosphate analogue 5 was found to be a weakly binding inhibitor, rather than a substrate, of the yeast transferase (12% inhibition at a concentration of 0.1 mmol L–1).Key words: glucose 1-phosphate, inhibition, UTP:α-D-glucose-1-phosphate uridylyltransferase.

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