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Abstract This thesis contains the following sections: 1-Introduction: It contains a survey covering different antibacterial and antifungal drugs, quinoline biological uses, chemistry of quinolines and a brief introduction about the ligand base pharmacophore modeling. 2-Research Objectives: It includes the design of 5,7 diiodo-8- hydroxyquinoline quinoline dervatives as antibacterial and antifungal agents. 3-Theoritical Discussion of experimental work : It includes different methods of preparation that are reported in literature which were used for the preparation of the intermediate and final compounds. 4- Microbiological evaluation: 22 newely synthesized compounds were evaluated as antibacterial and antifungal agents against two bacterial and two fungal strains. 5-Molecular Modeling: This part discusses the ligand base pharmacophore modeling to obtain a qualitative common feature hypothesis for antifungal agents and the fit values of the newly synthesized compounds. 6-Experimental: It contains methods used in preparation of compounds and the different conditions of each reaction. The structures of these compounds were confirmed by microanalytical and spectral data. This thesis comprises the synthesis of the following reported intermediates: 1- 1-(5,7-diiodoquinolin-8-yloxy)propan-2-one (IX). 2- Ethyl 2-(5,7-diiodoquinolin-8-yloxy)acetate (XV). 3- 2-(5,7-diiodoquinolin-8-yloxy)acetohydrazide (XVIII). Furthermore, the study involves the synthesis of the following new targeted compounds: 1- Ethyl 2-(5,7-diiodoquinolin-8-yloxy) propanoate (IIa). 2- Ethyl 3-(5,7-diiodoquinolin-8-yloxy) propanoate (IIb). 3- 2-(5,7-diiodoquinolin-8-yloxy ) propanoic acid (IIIa). 4- 3-(5,7-diiodoquinolin-8-yloxy ) propanoic acid (IIIb). 5- 2-(5,7-diiodoquinolin-8-yloxy) propanehydrazide (IV). 6-2-(5,7-diiodoquinolin-8-yloxy)-1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-1-one (V). 7- 1-(2-(5,7-diiodoquinolin-8-yloxy)propanoyl)-3-methyl-1H-pyrazol-5(4H)-one (VI). 8- 2-(5,7-diiodoquinolin-8-yloxy)-N-(1,3-dioxoisoindolin-2-yl)propanamide (VII). 9- 2-(5,7-diiodoquinolin-8-yloxy)-N-(2,5-dioxopyrrolidin-1-yl)propanamide (VIII). 10- 6-((5,7-diiodoquinolin-8-yloxy)methyl)-4-(4-fluorophenyl ) -1,2-dihydro-2-oxopyridine-3-carbonitrile (Xa). 11- 6-((5,7-diiodoquinolin-8-yloxy)methyl)-4-(4-methoxy pheny)-1,2-dihydro-2-oxopyridine-3-carbonitrile (Xb). 12- 6-((5,7-diiodoquinolin-8-yloxy)methyl)-1,2-dihydro-2-imino-4-(3,4,5-trimethoxyphenyl)pyridine-3-carbonitrile (XI). 13- 1-(5,7-diiodoquinolin-8-yloxy)-4-phenylbut-3-en-2-one (XIIa). 14- 1-(5,7-diiodoquinolin-8-yloxy)-4-(4-fluorophenyl)but-3-en-2-one (XIIb). 15-1-(5,7-diiodoquinolin-8-yloxy)-4-p-tolylbut-3-en-2-one (XIIc). 16- 8-((4,5-dihydro-5-phenyl-1H-pyrazol-3-yl)methoxy)-5,7-diiodoquinoline (XIV). 17- 8-((4,5-dihydro-1,5-diphenyl-1H-pyrazol-3-yl)methoxy)-5,7-diiodoquinoline (XIII). 18-1- (2- (5,7- diiodoquinolin -8- yloxy) acetyl) thiosemicarbazide 19-2-(5,7-diiodoquinolin-8-yloxy) -N- (2-hydroxyethyl )acetamide 20- 2- (5,7- diiodoquinolin -8- yloxy)-N,N-bis(2-hydroxyethyl)acetamide. 21- 2-(5,7-diiodoquinolin-8-yloxy) -N’-(D-glucose) acetohydrazide (XIXa). 22- 2-(5,7-diiodoquinolin-8-yloxy) -N’- (D-xylose) acetohydrazide (XIXb). 23- 2-(5,7-diiodoquinolin-8-yloxy) -N’- (D-arabinose) acetohydrazide (XIXc). 24-2-(5,7-diiodoquinolin-8-yloxy) -N’- (D-mannose) acetohydrazide (XIXd). 25-2-(5,7-diiodoquinolin-8-yloxy)-N’- (D-galactose) acetohydrazide (XIXe). 26- (1,2,3,4,5-penta-O-acetyl-D-gluco) -(5,7-diiodoquinolin-8-yl)]acetohydrazide (XXa). 27- (1,2,3,4-tetra-O-acetyl-D-xylo) -(5,7-diiodoquinolin-8-yl)]acetohydrazide (XXb). 28- (1,2,3,4-tetra-O-acetyl-D-arbino) -(5,7-diiodoquinolin-8-yl)]acetohydrazide (XXc). 29- N’-(1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-2-(5,7-diiodoquinolin-8-yloxy)acetohydrazide 30- N’-(1- (morpholino methyl)-2-oxoindolin-3-ylidene)acetohydrazide 7-Final Conclusion. 8-References: This thesis includes 178 reference covering the time period from 1851 till 2011. |