DESIGN, SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF NEW METFORMIN DERIVATIVES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2017, Vol 9, Issue 1
Abstract
Objective: The purpose of this work was to enhance oral bioavailability of metformin by incorporation of different amino acid residues through the glycolic acid spacer.Methods: Two series of metformin derivatives (V a-e) and (VI a-e) were synthesized by incorporation of five amino acids (glycine, alanine, phenylalanine, proline and GABA amino butyric acid) and their methyl esters respectively into metformin through glycolic acid spacer and preliminary evaluation for the antihyperglycemic activity was carried out using streptozotocin-induced diabetic rats model.Results: In vivo anti-hyperglycemic activity of the final compounds (V a-e) and (VI a-e) showed that compounds (V b, V c, VI c and V e) produced higher percent of decrease in blood glucose level compared to metformin after 5 h of the treatment while compounds (VI b, VI c, V d, VI d, V e and VI e) showed profound effect after 24 h of the treatment. Although compounds (V a, VI a, V b and V c) showed a significant decrease in blood glucose level at 5 h but their effect diminished at 24 h. Compound (V e) showed higher anti-hyperglycemic effect than metformin and its effect continued up to 24 h.Conclusion: From this study, it was concluded that incorporation of these amino acids or their methyl esters maintained or enhanced the antihyperglycemic effect of metformin.Â
Authors and Affiliations
Monther F. Mahdi, Inam S. Arif, Najwan K. Jubair
Keywords
Related Articles
- EP ID EP575800
- DOI 10.22159/ijpps.2017v9i1.15250
- Views 61
- Downloads 0
BIOLOGICAL SCREENING OF ARAUCARIA COLUMNARIS
Objective: The present research is biological screening of aerial part of Araucaria columnaris (Araucariaceae). There were investigation for their antibacterial, antifungal, phytotoxic and cytotoxic activities of Dichlor...
AROMATASE INHIBITORS - TYPES AND ADVANTAGES
The role of aromatase inhibitors in the management of breast cancer has been promising as it markedly suppresses the production of estrogen. The inhibitors are very effective in postmenopausal women and used as the first...
A SYSTEMATIC REVIEW OF HEPATITIS VIRUS REVIEW STUDIES: A CASE OF HEALTH ECONOMIC EVALUATION ANALYSIS
Objective: Systematic reviews of economic analysis are necessary for assessing reports and making a decision. A systematic review of systematic reviews is mean of summarizing the current evidence across specialties of th...
CYTOTOXICITY EVALUATION OF TITANIUM AND ZINC OXIDE NANOPARTICLES ON HUMAN CELL LINES
Objective: In vitro cytotoxicity evaluation of titanium dioxide, 20 nm (TNP 20) and zinc oxide, 20 nm (ZNP 20) nanoparticles (NP) were tested on different types of human skin (HaCat), lung (A549), liver (Hep G2) and colo...
GC-MS ANALYSIS OF PHYTOCHEMICAL CONSTITUENTS IN LEAF EXTRACTS OF NEOLAMARCKIA CADAMBA (RUBIACEAE) FROM MALAYSIA
Neolamarckia cadamba is one of the medicinal plants used in the treatment of various diseases traditionally. This study was conducted to identify the phytochemical constituents of N. cadamba leaf extracts using gas chrom...