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
Hauptverfasser: Kumar, Atul, Maurya, Ram Awatar, Sharma, Siddharth, Ahmad, Pervez, Singh, A.B., Bhatia, Gitika, Srivastava, Arvind K.
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container_end_page 6451
container_issue 22
container_start_page 6447
container_title Bioorganic & medicinal chemistry letters
container_volume 19
creator Kumar, Atul
Maurya, Ram Awatar
Sharma, Siddharth
Ahmad, Pervez
Singh, A.B.
Bhatia, Gitika
Srivastava, Arvind K.
description 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.
doi_str_mv 10.1016/j.bmcl.2009.09.031
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source MEDLINE; Elsevier ScienceDirect Journals
subjects Animals
Anti-dyslipidemic
Anti-hyperglycemic
Biological and medical sciences
Blood Glucose
Diabetes Mellitus, Experimental - blood
Diabetes Mellitus, Experimental - drug therapy
Dyslipidemias - blood
Dyslipidemias - drug therapy
General and cellular metabolism. Vitamins
Hypoglycemic Agents - classification
Hypoglycemic Agents - therapeutic use
Lipid Metabolism - drug effects
Medical sciences
Mice
Mice, Inbred C57BL
Pharmacology. Drug treatments
PPAR gamma - metabolism
PTP 1B
Pyranocoumarins
Pyranocoumarins - metabolism
Pyranocoumarins - therapeutic use
Rats
Rats, Wistar
Structure-Activity Relationship
title Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents
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