Imidazole derivatives of 1,4-naphthoquinones are found to have biological activity which interferes with the utilization of vitamin K or of the purines since they have groups common to these two classes of compounds. This thesis shows the preparation of some 1-substituted-naphthimidazole-4,9-diones for possible biological activity.

No description available.

Diss. (sammanfattning) Stockholm : Karolinska institutet, 2005. / Härtill 4 uppsatser.

Thesis (Ph. D.)--University of Wisconsin--Madison, 1960. / Typescript. Vita. eContent provider-neutral record in process. Description based on print version record. Includes bibliographical references.

No description available.

Submitted in fulfilment of the requirements of the Degree of Master of Technology: Chemistry, Durban University of Technology. 2014. / In this study, we report the synthesis of three quinolone bearing imidazole derivatives 2, 3 and 4 and two quinolone bearing BODIPY dyes 5 and 7. In the synthesis of 2, 3 and 4, the first step was the preparation of the starting compound 2-chloro-3-formyl quinoline (1); the Vilsmeier-Haack cyclisation protocol was used. Compound 1 was used with the appropriate diamine, together with POCl3 to produce 2, 3 and 4. These compounds were characterized by IR, 1H-NMR and 13C-NMR. In the synthesis of 5, compound 1 was used whilst 6 was used for the synthesis of 7. This was via. a one-pot synthesis using conventional reflux apparatus and Schlenk technique. These compounds were characterized by IR, 1H-NMR and 13C-NMR. Four other BODIPY dyes were also synthesized but their purification by column chromatography were unsuccessful. However a HPLC method was developed using 2 as a model; the best eluting solvent was 65 % methanol. After synthesis, 2, 3, 4, 5 and 7 were used for spectroscopic studies by UV-visible and fluorescence spectroscopy. In the UV-visible studies, 2, 3 and 4 were dissolved, separately, in five solvent viz. ethanol, methanol, dichloromethane, chloroform and acetonitrile. The UV profile of each compound was obtained and the maximum absorbance was then used for fluorescence studies. In the fluorescence studies, all the compounds displayed a fluorescence nature when excited with the various wavelengths. The fluorescence properties, namely Stoke shift, quantum yield, life time, molar absorptivity and brightness, were investigated to establish the properties of each compound in all five solvent systems. The Stoke shift was evident in all compounds and the quantum yields were below one which indicates no other electron transfer mechanisms occurring. The results displayed a favorable response and this further lead to analysis of the synthesized compounds for it potential application as a chemosensor. Eight metal ions were used to investigate this property. All eight metal ions, when reacted with the synthesized compounds, as ligands, showed chemosensor properties, viz. photon induced electron transfer, inter-molecular charge transfer and fluorescence resonance electron transfer, as a quenching and enhancement of emission and excitation peaks were observed. The compounds were further investigated for its potential for its use as a photovoltaic cells. The energies of the compounds were obtained from the analyses of the reflectance and transmission spectra. It was found that the synthesized compounds displayed properties which were positive for its use as a photovoltaic cell. Biological analyses using molecular docking analyses and MTT assays were conducted to determine the use of these as an anti-cancer drug. Compounds 2 and 3 formed hydrogen bonds with GLU 25 and LEU 27, respectively with MDM2-p53 proteins. Following the molecular docking studies, the MTT assay was performed on all five synthesized compounds. The BODIPYs with the quinoline moieties demonstrated a reduction in the rate of A549 cell proliferation when compared to the imidazole and benzimidazoles; this was observed for compounds 5 and 7. Further, a comparison between imidazoles clearly shows that compounds 3 and 4 also decreased cell proliferation. In contrast compound 2 exhibited an increased rate of cell proliferation. The optical density of the control cell, is much higher that the plates for concentration 31.25 µg/ mL to 500 µg/ mL. However 2 cannot be discarded; this compound clearly shows that it possesses anti-hyperglycaemic properties and further studies are recommended.

Wang, Yang. / "October 2011." / Thesis (M.Phil.)--Chinese University of Hong Kong, 2012. / Includes bibliographical references (leaves 87-92). / Abstracts in English and Chinese. / Acknowledgement --- p.I / Abstract (in English) --- p.III / Abstract (in Chinese) --- p.IV / Abbreviation --- p.V / List of Compounds --- p.VI / List of Figures --- p.IX / Contents --- p.X / Chapter Chapter 1 --- Introduction --- p.1 / Chapter 1.1 --- Synthesis and Structure of Half-Sandwich Group 4 Metallocarboranes Containing the Dicarbollyl Ligand --- p.2 / Chapter 1.2 --- Half-Sandwich Group 4 Metallacarboranes Catalyzed Reactions --- p.20 / Chapter 1.2.1 --- Polymerization of Olefins --- p.20 / Chapter 1.2.2 --- Catalytic Dimerization and Hydrogenation of Alkynes --- p.22 / Chapter 1.2.3 --- Catalytic Addition of Amines to Carbodiimides --- p.23 / Chapter 1.2.4 --- Catalytic Transamination of Guanidines --- p.24 / Chapter 1.2.5 --- Catalytic Synthesis of A^-Heterocycles --- p.25 / Chapter 1.3 --- Research Objectives of This Thesis --- p.26 / Chapter Chapter 2 --- Half-Sandwich Group 4 Metallacarborane Monoamindes --- p.27 / Chapter 2.1 --- Introduction --- p.27 / Chapter 2.2 --- Synthesis of Dicarbollyl Ligands Bearing Functional Side Arms --- p.27 / Chapter 2.3 --- Synthesis and Characterization of Half-Sandwich Group 4 Metallacarborane Monoamindes --- p.33 / Chapter 2.4 --- Summary --- p.43 / Chapter Chapter 3 --- Synthesis of 2-Aminoimidazoles Catalyzed by Half-Sandwich Titanacarborane Monoamide --- p.44 / Chapter 3.1 --- Introduction --- p.45 / Chapter 3.2 --- Known Methods for the Synthesis of 2-Aminoimidazole --- p.44 / Chapter 3.2.1 --- Condensations Methods --- p.44 / Chapter 3.2.2 --- Direct Introduction of N at C2 Position --- p.46 / Chapter 3.2.3 --- Heterocyclic Exchange Reactions --- p.47 / Chapter 3.2.4 --- Transition Metal Catalyzed Reactions --- p.48 / Chapter 3.3 --- Results and Discussion --- p.49 / Chapter 3.3.1 --- Synthesis of Propargy 1 Amines --- p.49 / Chapter 3.3.2 --- Synthesis and Characterization of 2-Aminoimidazoles --- p.50 / Chapter 3.3.3 --- Proposed Reaction Mechanism --- p.55 / Chapter 3.4 --- Summary --- p.57 / Chapter Chapter 4 --- Conclusion --- p.59 / Chapter Chapter 5 --- Experimental Section --- p.61 / References --- p.87 / Appendix / Chapter I. --- Publication Based on the Research Findings --- p.93 / Chapter II. --- Crystal Data and Summary of Data Collection and Refinement --- p.94 / Chapter III. --- X-ray crystallographic data in CIF (electronic form)

Diss. (sammanfattning) Stockholm : Karol. inst., 2004. / Härtill 4 uppsatser.

Thesis (Ph. D.)--University of Wisconsin--Madison, 1956. / Typescript. Vita. eContent provider-neutral record in process. Description based on print version record. Includes bibliographical references (leaves 92-96).

Construction of chiral complex molecules continues to be a challenge for organic chemists all over the world and to address this challenge numerous methodologies have been developed. 1,3-Dipolar cycloaddition reactions is one such simple and elegant method, which can be employed towards the construction of chiral heterocycles. The ability to construct multiple stereocenters in one operation is one of the salient features of dipolar cycloaddition reaction. Asymmetric dipolar cycloaddition via chiral Lewis or Bronsted acid catalyzed processes is aided by the development of various templates, which provide points of attachment for these catalyst. Application of acyl imidazoles as multifunctional templates has been investigated for Lewis and Bronsted acid catalyzed 1,3-dipolar cycloaddition of azomethine imines and nitrones. Chapter 1. A review of 1,3-dipolar cycloaddition towards to construction of chiral nitrogen containing heterocycles is discussed in this chapter. This chapter intends to provide the reader a current state of asymmetric 1,3-dipolar cycloaddition. Chapter 2. Development of exo and enantioselective Cu(II) catalyzed azomethine imine cycloaddition to pyrazolidinone acrylates is discussed in this chapter. The key issues approached in this chapter includes impact of metal geometry on diastereoselectivity as well as effect of N-l and C-5 substitution on enantioselectivity of cycloadducts. Investigation into the scope and limitation of azomethine imines and dipolarophiles has also been discussed. Chapter 3. This chapter introduces acyl imidazoles as multifunctional template for asymmetric azomethine imine cycloaddition. Limitation of substrate scope for azomethine imine cycloaddition encountered in the previous chapter has been resolved by the use of acyl imidazoles as templates. Synthesis of complementary diastereomers of azomethine imine cycloadducts via Lewis acid and Bronsted acid catalyzed reactions has been discussed in this chapter. Chapter 4. This chapter highlights the application of acyl imidazoles as template for first Bronsted acid catalyzed exo and enantioselective nitrone cycloaddition to electron deficient olefins. Study of appropriate chiral Bronsted acid and investigation of breadth and scope of nitrones and dipolarophiles has also been discussed here. Chapter 5. This chapter address one of the most challenging aspect of synthetic organic chemistry namely the construction of chiral quaternary stereocenters. This study highlights chiral Bronsted catalyzed nitrone cycloaddition to p,|3-disubstituted-a,P-unsaturated acyl imidazole leading to the formation of isoxazolidines with chiral quaternary stereocenter. This methodology is useful for the construction of chiral fluorinated heterocycles.