Post-synthetic conversion of 5-pivaloyloxymethyluridine present in a support-bound RNA oligomer into biologically relevant derivatives of 5-methyluridine

2017 ◽  
Vol 15 (9) ◽  
pp. 2097-2103 ◽  
Author(s):  
Karolina Bartosik ◽  
Elzbieta Sochacka ◽  
Grazyna Leszczynska

A reliable post-synthetic method to access the modified RNA oligomers containing biologically important 5-methyluridines: mnm5U, cmnm5U, τm5U, nm5U, inm5U and cnm5U.

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1813
Author(s):  
László Kollár ◽  
Ádám Erdélyi ◽  
Haroon Rasheed ◽  
Attila Takács

The aminocarbonylation of various alkenyl and (hetero)aryl iodides was carried out using tropane-based amines of biological importance, such as 8-azabicyclo[3.2.1]octan-3-one (nortropinone) and 3α-hydroxy-8-azabicyclo[3.2.1]octane (nortropine) as N-nucleophile. Using iodoalkenes, the two nucleophiles were selectively converted to the corresponding amide in the presence of Pd(OAc)2/2 PPh3 catalysts. In the presence of several iodo(hetero)arenes, the application of the bidentate Xantphos was necessary to produce the target compounds selectively. The new carboxamides of varied structure, formed in palladium-catalyzed aminocarbonylation reactions, were isolated and fully characterized. In this way, a novel synthetic method has been developed for the producing of N-acylnortropane derivatives of biological importance.


SynOpen ◽  
2018 ◽  
Vol 02 (02) ◽  
pp. 0161-0167
Author(s):  
Magdalini Matziari ◽  
Yixin Xie

A simple and efficient synthetic method towards α-substituted acrylic esters has been developed using the Horner–Wadsworth–Emmons (HWE) reaction with HCHO after alkylation of phosphonoacetates in a one-pot reaction. This method allows the smooth introduction of various side-chains, such as natural amino acids and other biologically relevant substituents. The use of mild conditions, inexpensive reagents, short reaction times and simple work-up and purification steps provides an effective and general alternative to cumbersome multistep and low-yielding procedures described to date.


2019 ◽  
Vol 48 (31) ◽  
pp. 11829-11837 ◽  
Author(s):  
Agnieszka Starobrat ◽  
Tomasz Jaroń ◽  
Wojciech Grochala

New derivatives of scandium borohydride have been prepared in a pure form using a facile synthetic method and physicochemically characterized.


1977 ◽  
Vol 8 (20) ◽  
pp. no-no
Author(s):  
YU. G. GOLOLOBOV ◽  
L. I. NESTEROVA

Molecules ◽  
2014 ◽  
Vol 19 (4) ◽  
pp. 4076-4082
Author(s):  
Karem Shanab ◽  
Catharina Neudorfer ◽  
Wolfgang Holzer ◽  
Markus Mitterhauser ◽  
Wolfgang Wadsak ◽  
...  

2016 ◽  
Vol 18 (13) ◽  
pp. 9281-9294 ◽  
Author(s):  
G. L. Perlovich ◽  
T. V. Volkova ◽  
A. V. Sharapova ◽  
V. P. Kazachenko ◽  
N. N. Strakhova ◽  
...  

Eight adamantane derivatives of sulfonamides were synthesized and characterized.


2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.


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