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Lysine-Vasopressin Analogues with Glycoconjugates in Position 8

100%

Marcinkowska A. , Borovickova L. , Slaninova J. , Grzonka Z.

2006

tom Vol. 80, nr 5

759-766

Two analogues of lysine-vasopressin in which the lysine side chain was modified by the attachment of glucuronic acid through the amide bond were synthesized and their pharmacological properties evaluated. In comparison to arginine-vasopressin used as a standard, both analogues were found to exhibit low activity in vasopressor test, moderate activity in antidiuretic test, and comparable activity in uterotonic test.

Engineered atenolol-glycoconjugates to target H9c2 cardiomyocyte cell lines

75%

Kumbha S. T. , Bhatia M. S. , Patil S. S.

tom no. 43

36--43

Background: One of the most important fields of biomedical engineering study nowadays is targeted drug delivery to specific cells. A drug's therapeutic efficacy can be improved and optimised by tightly targeting it to a pathophysiologically essential tissue architecture. The goal of this research is to develop saccharide conjugates for the targeted delivery of Atenolol, a -blocker. Methods: Galactose (monosaccharide), pectin (polysaccharide), and chitosan were chosen as the saccharides (polysaccharide). By grafting Atenolol with the modified saccharides, the conjugates were created. Spectroscopic and thermal studies were used to describe the chemically changed saccharides conjugates. H9c2 cell lines were used to conduct drug release research and cellular uptake studies. To investigate cytotoxicity, a brine shrimp lethality test was done. Results: The outcomes exhibit that Atenolol-modified saccharide conjugates can productively convey the medication to the target. Conclusion: It can be inferred that the improvement of saccharide-drug conjugates can be a compelling methodology for targeting cardiovascular medication.

Synteza i zastosowanie nowych katalizatorów metatezy olefin

63%

Hryniewicka A.

tom [Z] 68, 11-12

961--980

Olefin metathesis has emerged as a powerful tool for the formation of carboncarbon double bonds. The success of this methodology has spurred the intense investigation of new catalysts showing a better application profile. The syntheses and the application profiles of the seven new ruthenium metathesis catalysts have been described. Five of them were modified in benzylidene part with 6-hydroxychromane- and 2H-3,4-chromenemethylidene moiety. In chromanol – α-tocopherol model compound, some specific stereoelectronic effects have been observed. Introduction of this ligand to the catalyst may provide new advantageous properties. The other new catalysts contained modified N-heterocyclic carbene ligand (NHC), in which N,N’-mesityl substituents of NHC system were linked with diethylene glycol chain as a “clamping ring”. This ring would contribute to a steric shield of the NHC and ruthenium coordination center. Probably it may inforce a proper orientation of substituents in metallacyclobutane (all-cis), leading to Z-olefin formation. The obtained catalysts were investigated in model reactions: ring closing metathesis, cross metathesis and enyne metathesis. The experiments proved they efficiency. In many reactions the catalysts showed activity comparable or superior to that of commercially available Grubbs and Hoveyda 2nd generation complexes. Stereochemistry Z/E of the cross-metathesis products obtained using new and known complexes were similar as well. The catalysts were applied in the synthesis of a new type of α-tocopherol glycoconjugates. An efficient method of the synthesis Hoveyda 2nd type complexes starting from ruthenium trichloride was developed. It is possible to circumvent using special laboratory equipment and expensive reagents. Hoveyda type complexes can be achieved with very good yield in gram scale. Keywords: