NDLI: Complex formation of cyclodextrins with some pharmacologically active 1,2,4-thiadiazole derivatives : Thermodynamics and binding mode

Content Provider	Springer Nature Link
Author	Chislov, Mikhail Silyukov, Oleg Kumeev, Roman Proshin, Alexey Perlovich, German Terekhova, Irina
Copyright Year	2016
Abstract	Previously synthesized 1,2,4-thiadiazole derivatives displayed an activity in the treatment of Alzheimer’s disease; however, these compounds are poorly soluble in aqueous solutions. Inclusion complex formation with cyclodextrins is proposed for the development of water-soluble dosage forms of 1,2,4-thiadiazoles under study. To this end, binding of 1,2,4-thiadiazole derivatives with α-, β- and γ-cyclodextrins as well as with modified β-cyclodextrins was investigated by isothermal titration calorimetry, $^{1}$H NMR and UV–Vis spectroscopy in aqueous buffered solution (pH = 7.4) at 298.15 K. The detailed analysis of the thermodynamic parameters of complex formation is presented. The structure of 1,2,4-thiadiazole/cyclodextrin complexes was evaluated on the basis of 2D $^{1}$NMR (ROESY) experiments. The influence of structural factor (dimensions of macrocyclic cavity, modification of the host external surface, structure of guest molecules) on the thermodynamics and binding mode was discussed.
Starting Page	1797
Ending Page	1805
Page Count	9
File Format	PDF
ISSN	13886150
Journal	Journal of thermal analysis
Volume Number	127
Issue Number	2
e-ISSN	15882926
Language	English
Publisher	Springer Netherlands
Publisher Date	2016-11-08
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Cyclodextrins 1,2,4-Thiadiazole Alzheimer’s disease Complex formation Isothermal titration calorimetry $^{1}$H NMR Physical Chemistry Analytical Chemistry Polymer Sciences Inorganic Chemistry Measurement Science and Instrumentation
Content Type	Text
Resource Type	Article
Subject	Physical and Theoretical Chemistry Condensed Matter Physics

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