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DPP-IV INHIBITORS
 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
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
 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
 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
♦ 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
 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).
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).

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Introduction to DPP4 inhibitors in the treatment of Diabetes Mellitus.pptx

  • 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).