الفهرس 
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Abstract
In this thesis we aimed to synthesize some new heterocyclic compounds containing indole and assess their function for biological activity screening. Part (I): The reactivity of 3-(1H-indol-3-yl)-3-oxopropanenitrile (1) towards different diazonium salts was investigated. Thus, compound 1 was coupled smoothly with diazonium salts 2a-j to afford the corresponding hydrazones 3a-j, respectively. Condensation of aryl hydrazones 3d,e with malononitrile afforded the dihydropyridazines 5d,e via intermediacy of 4d,e. Formation of 5d,e is achieved by losing H20 and subsequent cyclization of the intermediate 4d,e. The Electronic Absorption Spectra of Compounds 3a-j. i) Effect of solvents. ii) Effect of substituent. iii) Effect of pH. Part (II): Enaminonitriles are important intermediates for the preparation of heterocyclic compounds possessing diverse biological activities. Enaminonitrile 4 reacted with 1,3-indandione to afford compound 5. The behavior of the enaminonitrile 4 towards an active methylene group incorporated into heterocyclic rings has been also studied, cycloaddition of 4 with barbituric acid in glacial acetic acid afforded the pyrano[2,3-d]pyrimidine derivative 6. It was of interest to investigate the reactivity of the enaminonitrile 4 towards dimedone in refluxing glacial acetic acid yielded the coumarine derivative 12. It was of interest to synthesize 6-(1H-indole-3-carbonyl)-8,8a-dihydro-5H-thiazolo[3,2-a]pyrimidin-5-one (16) by treatment of compound 4 with 2-aminothiazole in boiling glacial acetic acid furnished 16 were considered. Part (III): Reaction of compound 1 with carbon disulfide in dilute hydrochloric acid to afford 2-cyano-3-(1H-indol-3-yl)-3-oxopropanedithioic acid (19). For preparing thiophene derivatives 28 we added N,N- dimethylformamide in the presence of a catalytic amount of TEA for the acyclic product 27. In a similar manner, refluxing 1 with 2-mercaptoethan-1-ol in N,N-dimethylformamide dimethylacetal with a few drops of peperidine led to the formation of compound 33. PART (IV): 1) Fourteen of the newly synthesized target compounds (3a-j, 5d,e, 7d,e) were evaluated for their in vitro antibacterial activity against Gram-positive bacteria and Gram-negative bacteria and the results showed that most of the tested compounds revealed better activity against the Gram-positive rather than the Gram- negative bacteria. 2) Compounds 3h and 7d were equipotent to Chloramphenicol and Ampicillin in inhibiting the growth of B. Subtilis (MIC 3.125 mg/mL), while its activity was 50% lower than of Chloramphenicol against B. Thuringiensis. 3) The activity of azo derivatives against antifungal strains revealed that compounds 3b, 3d and 3h were 50% lower than Cycloheximide in inhibitory the growth of B.Fabae and F.Oxysporum (MIC 6.25 mg/ml).