2. Diabetes is one of the most significant public
health challenges that we face in the 21st century.
Diabetes is a silent killer, 3.5 million deaths are
attributable to diabetes each year, yet the disease
goes largely ignored. Diabetes kills as many
people each year as HIV/AIDS.
Diabetes Mellitus
3. A. Insulin
B. Oral hypoglycemic drugs:
Insulinsecretagogues ‘
1. Sulfonylurea drugs ‘
2. Meglitinide analogues ‘
3. D-phenylalanine derivatives
Insulinsensitizers ‘
1. Biguanides ‘
2. Thiazolidinediones
C. Alpha glucosidase inhibitors
D. Gastrointestinal hormones ones or glitazones
Antidiabetics drugs
4. Introduction
Incretin hormones, such as GLP-1. These are rapidly
secreted from the gut following food intake.
GLP-1 is responsible for metabolism of glucose and
glucose reuptake from body.
DPP-IV Inhibitors
5.
6.
7.
8.
9. Within 1-2 minutes only ;80% Glp-1 active converts to
GLP-1 inactive form.
This happened by DPP4.
TO GET MORE BENEFITS OF INTERNAL we have to :
1)Prolong the half life
2)Decrease the amount of inactivity
Inhibition of DPP-4 Increases Active GLP-1
10. ♦ Once daily ingestion Once daily ingestion
♦ Reduce fasting and postprandial glucose,
♦ Decrease glucagon response to ingested meal
♦ Initial studies in combination with metformin
DPP- IV Inhibitors
11. DPP-4 inhibitors eg: sitagliptin, saxagliptin, linagliptin,
omarigliptin are a class of drugs that prolong the
action of incretin hormones. DPP-4 degrades
numerous biologically active peptides, including
including the endogenous incretins GLP-1 and
glucoseendogenous insulinotropic polypeptide
dependent insulinotropic polypeptide (GIP).
12. Bibliography
Bibliography:
Diabetes Mellitus: Marked improvement in carbohydrate and lipid metabolism in diabetic
Australian Aborigines after temporary reversion to traditional lifestyle. 1984; 33: 596-603.
A Convenient Synthesis Of Coumarins Using Reusable Ionic Liquid As Catalyst, Chapter I,
Section II
Gang Qi, Wenguo Zhang. Synthesis of New Coumarin Compounds and Its Hypoglycemic
Activity and Structure-Activity Relationship in Asian journal of Chemistry, 2013 Vol 25 No. 17,
9835- 9839.
Abha Kathuria, Sarah Jalal. Substituted Coumarin Derivatives: Synthesis and Evaluation of
Antiproliferative and Src Kinase Inhibitory Activities in Chemistry & Biology Interface, 2011, 1,
2, 279-296.
Swayam Sourav Sahoo, Smita Shukla, Subhangankar Nandy, Himanshu Bhusan Sahoo. Synthesis
of novel coumarin derivatives and its biological evaluations in European Journal of Experimental
Biology, 2012, 2 (4):899-908.
Rina Soni, Sunil Dutt Durgapal, Shubhangi S. Soman, John J. Georrge . Design, synthesis and
antidiabetic activity of chromene- 2- one derivatives in Arabian journal of Chemistry (2016).