I= SYNTHESIS AND SYNTHETIC TRANSFORMATION OF HETEROCYCLIC COMPOUNDS AND NATURAL PRODUCTS IN SEARCH OF USEFUL THERAPEUTIC AGENTS
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Title of Thesis
SYNTHESIS AND SYNTHETIC TRANSFORMATION OF HETEROCYCLIC COMPOUNDS AND NATURAL PRODUCTS IN SEARCH OF USEFUL THERAPEUTIC AGENTS

Author(s)
Zia Ullah
Institute/University/Department Details
University of Karachi/H.E.J Research Institute of Chemistry
Session
2004
Subject
Chemistry
Number of Pages
223
Keywords (Extracted from title, table of contents and abstract of thesis)
heterocyclic compounds, therapeutic agents, heterocycles, enzyme inhibition, thiophenes

Abstract
This dissertation synthesis and synthetic transformation of different classes of heterocycles such as 2,5-disubstituted-1,3,4-oxadiazoles, 2-substituted-1,3, thiazolidines-4-carboxylic acid, 2-aminothiophenes and their analogs in search of important therapeutic agents.

Some 2,5-disubstituted-1,3,4-oxadiazoles have been synthesized and found to be novel tyrosine inhibitors. 2-Substituted-1,3-thiazolidines-4-carboxylic acid and 2-aminothiophenes have been discovered as potential urea inhibitors.

Some hydrazides were screened for their in vitro leishmanicidal activity and have been found to have very exciting activities. Leishmaniasis, which is endemic to eighty two countries throughout the world and is most frequent in south east region, has been reviewed extensively.

This dissertation also deals with a new emerging microwave assisted synthetic methodology and its use in the synthesis of various compounds of therapeutic importance.

In addition to above all this dissertation describes the exciting four step “total synthesis of (4S,5R)-(+)-L-Factor, also called as (SS)-5-[(IR)-1-hydroxyhexy1]dihydro-2(3H)-furanone, a proposed autoregulator of anthracycline biosynthesis” from commercially available L-glutamic acid [(S)-(+)-glutamic acid].

The chemistry of the CsF-Celite has also beenexploited because it can serve as an excellent solid base for converting carboxylic acid into their corresponding esters with alkl halides. A methodology based on CsF-Celite has also been developed to synthesize y-lactone skeleton.

Download Full Thesis
1886.95 KB
S. No. Chapter Title of the Chapters Page Size (KB)
1 0 Contents
174.15 KB
2 1 CHAPTER 1 1
337.94 KB
  1.1 Summary 7
  1.2 Enzyme Inhibition 11
3 2 CHAPTER 2 15
607.19 KB
  2.1 Introduction 35
4 3 CHAPTER 3 30
399.22 KB
  3.1 Introduction 106
  3.2 Results and Discussion 115
  3.3 Biology 140
  3.4 Experimental 135
5 4 CHAPTER 4 140
299.76 KB
  4.1 Thiophenes 155
  4.2 Results and Discussion 159
  4.3 Experimental 177
6 5 CHAPTER 5 160
113.08 KB
  5.1 Introduction 188
  5.2 Results and Discussion 190
  5.3 Synthetic Strategy 190
  5.4 Experimental Section 195
7 6 CHAPTER 6
229.29 KB
  6.1 Introduction 199
  6.2 Results and Discussion 200
  6.3 Experimental 204
  6.4 Research Articles 221
  6.5 References 219