scholarly journals Synthetic Route to Glycosyl β-1C-(phosphino)-phosphonates as Unprecedented Stable Glycosyl Diphosphate Analogs and Their Preliminary Biological Evaluation

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4969
Author(s):  
Michaël Bosco ◽  
Su-Jin Paik ◽  
Patricia Busca ◽  
Stuart E. H. Moore ◽  
Christine Gravier-Pelletier
Keyword(s):  
Alkaline Phosphatase ◽  
Double Bond ◽  
Biological Evaluation ◽  
Synthetic Method ◽  
Synthetic Route ◽  
Stereoselective Addition

The synthesis of glycosyl-β-1C-(phosphino)-phosphonates is a challenge since it has not yet been described. In this paper, we report an innovative synthetic method for their preparation from Glc-, Man-, and GlcNAc- lactone derivatives. The proposed original strategy involves the addition of the corresponding δ-hexonolactones onto the dianion of (methylphosphino) phosphonate as a key step, followed by dehydration and stereoselective addition of dihydrogen on the resulting double bond. Final deprotection provides the new glycosyl diphosphate analogs in 35%, 36%, and 10% yield over 6 steps from the corresponding δ-hexonolactones. The synthetized compounds were evaluated as inhibitors of phosphatase and diphosphatase activities and found to have complex concentration-dependent activatory and inhibitory properties on alkaline phosphatase. The synthetized tools should be useful to study other enzymes such as transferases.

Size-tunable and scalable synthesis of uniform copper nanocrystals

RSC Advances ◽  
2015 ◽  
Vol 5 (4) ◽  
pp. 2756-2761 ◽  
Author(s):  
Hwansu Sim ◽  
Jihwan Lee ◽  
Taekyung Yu ◽  
Kyungpil Kim ◽  
Seong Jun Lee ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Synthetic Method ◽  
Synthetic Route ◽  
Scalable Synthesis

A facile and scalable synthetic route to uniform Cu nanocrystals with tunable sizes in the range of 20–100 nm based on an ethylene glycol-assisted synthetic method was developed.

scholarly journals Synthesis and Biological Evaluation of Furo[3,2-c]pyrazole-5-carbimidates

2019 ◽  
Vol 31 (10) ◽  
pp. 2389-2393
Author(s):  
Sravanthi Siliveri ◽  
Harinadha Babu Vamaraju ◽  
Shivaraj
Keyword(s):  
Antibacterial Activity ◽  
Double Bond ◽  
Spectral Data ◽  
Biological Evaluation ◽  
Significant Protection ◽  
Edema Formation ◽  
Anti Inflammatory ◽  
Alkoxy Groups ◽  
Oxidative Difunctionalization ◽  
Synthesis And Biological Evaluation

In the present work, novel pyrazole fused dihydrofurans synthesized via a chronological addition of N-chloro succinimide and base piperidine to pyrano[3,2-c]pyrazole carbonitrile derivatives in methanol medium. Oxidative difunctionalization was done with the reagent N-chloro succinimide by the addition of both chlorine and alkoxy groups crosswise the chromene double bond. The addition of base results in the construction of dihydrofuran derivatives by ring contraction. The structures of newly synthesized compounds were characterized on the basis of physical and spectral data. Synthesized compounds were evaluated for antibacterial and anti-inflammatory activities. All the compounds exhibited significant antibacterial activity against all the four strains of bacteria and their MICs ranged between 1.56 and 12.55 μg/mL. In anti-inflammatory screening, among all the tested compounds, compounds 7, 8, 9, 11, 12, 13, 14, 16, 17 and 18 exhibited significant protection against the edema formation at a concentration of 100 mg/kg.

Efficient and Eco-Friendly Synthesis of Fluorenone Azines by Using Sulphated Titania Acid Catalyst

2015 ◽  
Vol 58 ◽  
pp. 137-143 ◽  
Author(s):  
V. Arun ◽  
K.R. Sankaran
Keyword(s):  
Reaction Time ◽  
Acid Catalyst ◽  
Recyclable Catalyst ◽  
Synthetic Method ◽  
Synthetic Route ◽  
Operating Method

Conjugated unsymmetrical azines have been synthesized in the presence of acid catalyst sulphated-titania (TiO2-SO42-) from fluorenone hydrazone with substituted aldehydes and acetophenones by using mortar and pestle. The scope of present synthetic route avoid in solvents, simple operating method and shorter reaction time. Special feature of synthetic method is recyclable catalyst for all in reactions.

Highly stereoselective one-pot construction of trisubstituted tetrahydro-β-carboline-fused diketopiperazines: a synthetic route towards cialis analogues

RSC Advances ◽  
2014 ◽  
Vol 4 (72) ◽  
pp. 38159-38163 ◽  
Author(s):  
Mouhamad Jida ◽  
Dirk Tourwé ◽  
Steven Ballet
Keyword(s):  
Synthetic Method ◽  
Synthetic Route ◽  
One Pot

A facile and efficient synthetic method for the stereoselective preparation of trisubstituted tetrahydro-β-carboline-fused diketopiperazine derivatives is reported.

Electrochemically activated solid synthesis: an alternative solid-state synthetic method

2018 ◽  
Vol 47 (41) ◽  
pp. 14604-14611 ◽  
Author(s):  
Junnan Liu ◽  
Henrik Lyder Andersen ◽  
Othman K. Al Bahri ◽  
Saroj Bhattacharyya ◽  
Aditya Rawal ◽  
...  
Keyword(s):  
Solid State ◽  
Synthetic Method ◽  
Thermal Treatments ◽  
Synthetic Route ◽  
Electrochemical Discharge ◽  
Solid Synthesis

Electrochemical discharge followed by thermal treatments leads to the generation of unconventional phases upon heating, an alternative synthetic route.

Synthesis and Characterization of Novel (E)-4-(4-(((1,3-diphenyl-1H-pyrazol-4-yl)methylene)- amino)phenyl)morpholin-3-one Derivatives

2019 ◽  
Vol 4 (4) ◽  
pp. 236-239
Author(s):  
Krushnakumar J. Jilariya ◽  
P.K. Patel ◽  
Yogesh J. Sanghani ◽  
Vijay D. Chodvadiya ◽  
Jayesh Babariya
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Biological Evaluation ◽  
Synthesis And Characterization ◽  
Spectroscopic Techniques ◽  
Synthetic Route ◽  
Formation Reaction ◽  
Schiff Base Formation ◽  
Base Formation

A highly functionalized heterocyclic compounds series were synthesized, characterized and tested for biological evaluation against bacteria and fungus. This novel synthetic route involves Schiff base formation reaction of 1,3-diphenyl-1H-pyrazole-4-carbaldehyde with 4-(4-aminophenyl)morpholin-3-one in the presence of base and methanol as a solvent in good yield and high purity. All the synthesized compounds were characterized using IR, 1H NMR and mass spectroscopic techniques. All the compound screened for antimicrobial activity against standard drugs.

Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: Synthesis and biological evaluation

2011 ◽  
Vol 21 (2) ◽  
pp. 764-768 ◽  
Author(s):  
Ornella Mesenzani ◽  
Alberto Massarotti ◽  
Mariateresa Giustiniano ◽  
Tracey Pirali ◽  
Valentina Bevilacqua ◽  
...  
Keyword(s):  
Double Bond ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation
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