Gilli, Paola and Cvetkovski, Aleksandar (2016) Hydrogen-bonded cocrystals of the drug metformin: from molecular interactions analysis to supramolecular synthesis and characterization of Met-bis(DCA), a pharmaceutical cocrystal with enhanced anti-leukemic activity. Acta Crystallographica Section A, 72 (A72). p. 114. ISSN 2053-2733
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Abstract
Metformin (met) being a drug of first choice for oral therapy of type 2 diabetes, its anticancer activity is the subject of active research. Met can exist in three resonance-stabilized forms, i.e. as neutral molecule (Met), monoprotonated (MetH+) or diprotonated (MetH22+) cation, with dissociation
constants in water typical of biguanides: pKa1~12.40;
pKa2=2.96.
As successful application, we report the crystal
engineering, supramolecular synthesis, crystal structure
determination and in vitro biological activity testing of
two new PCCs of Met with the antileukemic drug
dichloroacetic acid (DCA, pKa=0.9) in 1:1 (1,
MetH+∙DCA-) and 1:2 (2, MetH2
2+∙2DCA-) ratio,respectively.
| Item Type: | Article |
|---|---|
| Subjects: | Medical and Health Sciences > Basic medicine Engineering and Technology > Chemical engineering Engineering and Technology > Nano-technology |
| Divisions: | Faculty of Medical Science |
| Depositing User: | Aleksandar Cvetkovski |
| Date Deposited: | 27 Jan 2017 11:06 |
| Last Modified: | 27 Jan 2017 11:06 |
| URI: | https://eprints.ugd.edu.mk/id/eprint/17058 |
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