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Title of Thesis  
PHARMACOLOGICAL ACTIVITY DRIVEN SYNTHESES OF ORGANIC COMPOUNDS  
Author(s)  
MAIMONA RASHEED  
Institute/University/Department Details  
University of Karachi, Karachi/Chemical Sciences  
Status (Published/ Not Published/ In Press etc)  
Published  
Date of Publishing  
April, 2001  
Subject  
Chemistry  
Number of Pages  
193  
   
Keywords (Extracted from title, table of contents and abstract of thesis)  
Organic compounds, 1,3,4-oxadiazole-2(3H0-thione, Enzyme, Urease, Leishmania, Antibacterial, [5,5-bi1,3,4-thiadiazole]-2,2’(3H,3H)-dithione, Pharmacologically active compounds, 1,3,4-oxadiazole-4H-5(6H), 4-amino-2,4-dihydro-3H-1,2,4-triazole-3-thione, 2-imidazoline,  

 

 
Abstract  

The research work reported in this dissertation is consists of synthesis of pharmacologically active compounds and the modification of their structure according to the result of pharmacological screening. All these synthesized compounds were identified by the satisfactory spectroscopic data. These compounds belongs to the classes 1,3,4-oxadiazole-2(3H)-thione, 1,3,4- thiadiazole-2(3H)-thione, 1,3,4-oxadiazin-4H-5(6H)-one, 4-amino- 2,4-dihydro-3H-l,2,4-triazole-3-thione and 2-imidazoline. The biological activities associated with 1,3,4-oxadiazole-2(3H)-thione which initiate us to synthesize these heterocyclic compounds are discussed in chapter 1. All these compounds and some of their intermediates were screened for different biological activities including bactericidal, fungicidal, phytotoxic, cytotoxic, urease inhibitory activity and leishmanicidal activities and as expected most of them had exhibited moderate to good activities. The most important result is the evaluation of the 1, 3, 4- oxadiazole-2(3H)-thione, 1, 3, 4-thiadiazole-2(3H)-thione and 4- amino-4H-l, 2, 4-triazol-3-'thione as potential inhibitor of the enzyme urease. Urease is an ureolytic enzyme and is found to be virulence factor of many pathogenic microorganisms. Medicinally its inhibitors are important for the treatment of gastric ulceration, gastric carcinoma, urinary stone formation and pyelonephritis. The decomposition of the urea, the most commonly used fertilizer, by the urease of soil microorganism can also be controlled by urease inhibitors. The synthesized compounds are found to be irreversible inhibitor of urease and their IC50 values are found to be below than l00uM. The second achievement of this research is the discovery of hyrdrazides as potential leishmanicidal agent. The hydrazides that are intermediate in the synthesis of these heterocyclic compounds were screened for the leishmanicidal activity and are found to be the potent leishmanicidal agents. The IC10 value of the four most potent compounds was found to be below than 15 ug/ml.

 
   
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Sr.No Chapter Table of Contents
 
i 180.kbs
147.KB
1 1

INTRODUCTION

1
323.KB

1-        1,3,4-oxadiazole-2(3H)-thione

4

2-        Enzyme

11
3-        Urease 20
4-        Leishmania 24
5-        Antibacterial agents 31
2 2 RESULTS AND DISCUSSION 42
649.KB
7-        Bioassay techniques  
3 3 EXPERIMENTAL 107
865.KB
8-        General Experimental 107
9-        Chemistry 109
10-      Bioassay techniques 159
11-      Future plan 162
4 4 References 163
341.KB