Rasheed, Maimona (2001) PHARMACOLOGICAL ACTIVITY DRIVEN SYNTHESES OF ORGANIC COMPOUNDS. PhD thesis, University of Karachi, Karachi.
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.
|Item Type:||Thesis (PhD)|
|Uncontrolled Keywords:||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,|
|Subjects:||Physical Sciences (f) > Chemistry(f2)|
|Deposited By:||Mr Ghulam Murtaza|
|Deposited On:||16 Jun 2006|
|Last Modified:||04 Oct 2007 21:00|
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