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International Journal of Pharmaceutical Chemistry and Analysis


Development of Murrayanine-Chalcone hybrids: An effort to combine two privilege scaffolds for enhancing hypoglycemic activity


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Author Details: Debarshi Kar Mahapatra, Santosh S. Chhajed, Ruchi S. Shivhare

Volume : 4

Issue : 2

Online ISSN : 2394-2797

Print ISSN : 2394-2789

Article First Page : 30

Article End Page : 34


Abstract

Murrayanine and chalcone are well known for their anti-diabetic potentials. The present research represents an effort is represented in which the two scaffolds were rationally integrated with an objective that the designed hybrid molecule will cumulatively produce higher pharmacological activity than their parents, and will also illustrate analogous or more pronounced activity with the marketed product. All the novel murrayanine-chalcone hybrids exhibited activity in the range of 6.27-30.87%. The molecules 3a, 3f, 3g, and 3h exhibited an effective reduction of blood glucose level (>18%). Chalcone 3g, having two lipophilic substituents at meta positions in the B-ring presented the highest anti-hyperglycemic activity (30.87% lowering of glucose level). From the study, it was evidenced that the positions of substitution and their number played an intense role in exhibiting anti-diabetic activity. A superior biological activity was observed with electrophilic halogen substituents at para and meta positions as compared to ortho position. However, a very well defined structure-activity-relationship (SAR) cannot be defined from this study. The study opened new avenues for utilizing the natural scaffolds in form of hybrids as anti-diabetic agents which may act by modulating various anti-diabetic targets. Still, further research is needed to elucidate the complete mechanism of action(s) of the synthesized hybrids.

Keywords:
Murrayanine; Chalcone; Hybrid; Antihyperglycemic; Antidiabetic; Hypoglycemic.