الفهرس 
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Abstract
The target compounds of the present thesis stems from a quinoline-4-carboxylic acid. Therefore, it is noteworthy to mention some of the reported biological activities of quinoline-4-carboxylic acid and its derivatives as well as the different methods (protocols) of their synthesis.
Literature survey revealed that quinoline-4-carboxylic acid and its derivatives such as esters and amides display a broad range of biological activities. The profile of biological action depends on the nature of the substitutent around the core moiety(1) and it is known that position 2,3 and 6 of quinoline system are usually crucial for the manifestation of bioactivity(1-6).
Numerous derivatives of quinoline-4-carbohydrazides (3) were studied for their antitubercular activity. A series of 2,6-disubstituted quinoline-4-carbohydrazides was prepared and found to exhibit antitubercular activity(8).
A group of novel 8-chloro-2-heteroarylquinoline-4-carboxylic acids and their derivatives(4) were prepared and found to be useful as antibacterial agent, being especially useful in the treatment of infections of streptococcal origin(9).
A mild and facile method for the synthesis of 3-arylbenzo[f]quinoline-1,2-dicarboxylate derivatives(34) is reported by an imino-Diels-Alder reaction in high yields (76-92%). This procedure includes a novel three-component reaction of aromatic aldehyde(31), naphthalen-2-amine(32), and but-2-ynedioate(33) catalyzed by Yb(OTf)3 in toluene(45).
A new series of 2-arylquinoline-4-carboxylic acid hydrazide-hydrazones was synthesized. It was found that 6-chloro-2-(4-methoxyphenyl) quinoline-4-carboxylic acid (4-nitrobenzylidene)-hydrazide(7) to be the most potent among test hydrazones in which nitro group in the arylidene side chain generally enhances antifungal and antibacterial activity against E. coli , the same compound was assessed for hemolytic toxicity and found to be non-hemolytic up to a concentration of 100mg/ml(11).
A series of 2-arylquinoline derivatives (5) was prepared and evaluated for their antifungal activity. 2-(4-bromophenyl)quinoline-4-carboxylic acid was identified from high-throughput screening of library compounds. This compound was found to have antifungal activity through inhibiting prolyltRNAsynthetase. In addition, it has more than 200 fold selectivity for the fungal enzyme over the human enzyme. The 4-bromophenyl analogue was more potent than phenyl analogue. On other hand 2-(4-methoxy), 2-(4-trifluoromethyl) analogues showed a significant loss in potency compared with 2-(4-bromo) one. Replacement of the bromophenyl group by a heterocyclic group such as the 2-chlorothienyl group decrease the activity. The furyl analogue was inactive(10).