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Title: Design Synthesis and Biological Evaluation of Heterocycles Targeting Dipeptidyl Peptidase 4 DPP 4 for Management of Type 2 Diabetes
Researcher: Upadhyay, Jagat
Guide(s): Gajjar, Anuradha
Keywords: Clinical Pre Clinical and Health
Pharmacology and Pharmacy
Pharmacology and Toxicology
University: Nirma University
Completed Date: 2020
Abstract: newlineThe research work titled Design, Synthesis and Biological Evaluation of Heterocycles Targeting Dipeptidyl Peptidase-4 (DPP-4) for management of Type 2 Diabetes is divided into 7 chapters mentioned in brief as follows. newlineChapter 1 outlines historical aspects of diabetes, epidemiology, prevalence, classification and current therapies for management of Type 2 Diabetes (T2D). Novel therapies under development for management of T2D encompassing targets and related New Chemical Entities (NCEs) are described. newlineChapter 2 begins with role of incretin hormones in blood sugar control, effect of Dipetidyl Peptidase-4 (DPP-4) and impact of DPP-4 inhibition on blood sugar levels. It is followed by classification systems of DPP-4 inhibitors, Gliptins and discussion about peptidomimetic and non-peptidomimetic inhibitors with importance on diversity in their structure. Chapter is concluded with advantages and limitations of Gliptins. newlineAim of present work was envisaged to exploit computer-aided drug design approaches to identify new small molecules as DPP-4 inhibitors. Aim and objectives of the research work are briefed in chapter 3. newlineChapter 4 is detailed on various computational tools to identify new molecules that can inhibit DPP-4. In present work, various X-ray crystal structures of DPP-4 enzymes were analyzed to study their active site and interaction pattern. Following the virtual screening, methodologies were used for identification of new synthetic small molecules having the affinity for DPP-4 inhibitors. newlineCommon feature pharmacophore approach was used in combination with docking to screen the commercial compound library for searching new templates that may inhibit DPP-4, and few selected hits were subjected to in-vitro DPP-4 enzyme inhibition assay. Docking poses obtained for few hit compounds were confirmed by molecular dynamics simulation. In second computational approach molecular dynamics structure-based pharmacophore approach was used to generate receptor-based pharmacophore using multiple DPP-4 protein newlineiii newline
Appears in Departments:Institute of Pharmacy

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01_title.pdfAttached File34.19 kBAdobe PDFView/Open
02_certificate.pdf262.77 kBAdobe PDFView/Open
03_abstract.pdf41.14 kBAdobe PDFView/Open
04_declaration.pdf302.38 kBAdobe PDFView/Open
05_acknowledgements.pdf40.39 kBAdobe PDFView/Open
06_contents.pdf58.1 kBAdobe PDFView/Open
07_list of figures.pdf53.97 kBAdobe PDFView/Open
08_list of tables.pdf44.49 kBAdobe PDFView/Open
09_abbreviations.pdf59.55 kBAdobe PDFView/Open
10_chapter 1.pdf215.76 kBAdobe PDFView/Open
11_chapter 2.pdf332.34 kBAdobe PDFView/Open
12_chapter 3.pdf33.93 kBAdobe PDFView/Open
13_chapter 4.pdf3.27 MBAdobe PDFView/Open
14_chapter 5.pdf1.53 MBAdobe PDFView/Open
15_chapter 6.pdf231.45 kBAdobe PDFView/Open
16_chapter_7.pdf71.58 kBAdobe PDFView/Open
17_publications.pdf32.58 kBAdobe PDFView/Open
18_bibliography.pdf224.4 kBAdobe PDFView/Open
80_recommendation.pdf224.47 kBAdobe PDFView/Open
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