Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents
A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds 7a, 7c, 8a, 8b, 8c, 8e and 8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged s...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (22), p.6447-6451 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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Zusammenfassung: | A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds
7a,
7c,
8a,
8b,
8c,
8e and
8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds
8a and
8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds
8a (IC
50
=
24.5
μM) and
8b (IC
50
=
36.2
μM) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds
7a,
7b,
8a,
8b,
8d,
8e and
8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.09.031 |