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Pharmacokinetic Profiling of Some Carbohydrate Derivatives and Their Structure Activity Relationship Evaluation

[ Vol. 14 , Issue. 3 ]

Author(s):

Jovana Trifunovic*, Vladan Borcic*, Sasa Vukmirovic and Momir Mikov   Pages 262 - 270 ( 9 )

Abstract:


Background: Carbohydrates are of great interest for the synthesis of novel ribonucleosides and C-Nucleosides which often show different pharmacological potential including antiinflammatory and antineoplastic characteristics.

Introduction: In this research twelve aldopentose derivatives were examined and their chromatographic properties were used to describe their pharmacokinetic profiles.

Methods: Thin layer chromatography was performed using three mobile phases: acetone–water (φ = 0.5–0.7 v/v), dioxane–water (φ = 0.5–0.7 v/v) and methanol–water (φ = 0.5–0.7 v/v). Multiple linear regression was performed to examine correlation between lipophilicity and pharmacokinetic descriptors of the examined molecules.

Results: Good oral absorption can be expected for all investigated compounds. Moderate volume of distribution indicates low to moderate probability of their accumulation in body tissues. All investigated molecules show good pharmacokinetic characteristics but compounds 2, 3, 5, 6 and 7 demonstrated the best biological potential and biochemical activity such as inhibition of protease and kinase (compound 7) and possibility to be a ligand for GPCR.

Conclusion: Among the best candidates authors would emphasize structure 7 as the most promising molecule regarding its pharmacological potential.

Keywords:

Aldopentose, multiple linear regression, QSAR, pharmacokinetic, ADME, lipophilicity.

Affiliation:

Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad, Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, University of Novi Sad, Novi Sad

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