National Repository of Grey Literature 19 records found  1 - 10next  jump to record: Search took 0.01 seconds. 
Synthesis of tetrazoles as anticuberculotics
Vicherek, Petr ; Čonka, Patrik (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Vicherek Supervisor: RNDr. Patrik Čonka, Ph.D. Title of diploma thesis: Synthesis of tetrazoles as antituberculotics Although significant progress in therapy of tuberculosis has been made since effective drugs were discovered in the second half of the 20th century, it is still widespread and refractory curable disease. The situation is complicated with growing appearance of resistant strains and for that reason it is necessary to search for new potential antituberculotics. The aim of this work was to continue with synthesis of antimycobacterial-efficient structures based on tetrazole. Firstly, we synthesised derivates of 1-aryl-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazole by the method of Williamson's synthesis, when the reaction of 1-aryl-1H-tetrazol-5-thiol with 3,5-dinitrobenzylchloride was performed. Conditions of the reactions were further optimalised. We prepared by the same way derivates of 1-fenyl-5-[(3,4,5- trimethoxybenzyl)sulfanyl]-1H-tetrazole afterwards, as analogues of previous tetrazoles missing the electron withdrawing 3,5-dinitrosubstitution. Furthermore, we concentrated on synthesis of substituted 1,5-diphenyl-1H-tetrazoles. Substituted...
Synthesis of substituted pyridines catalyzed by gold complexes
Matouš, Petr ; Pour, Milan (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Matouš Supervisor: Prof. RNDr. Milan Pour, Ph.D. Title of thesis: Synthesis of substituted pyridines catalyzed by gold complexes This work is focused on the synthesis of 3,4-disubstituted pyridine derivatives. MBS-protected propargylamine reacts with methyl propiolate to form 1,5-enyne that undergoes Sonogashira coupling with aryl iodides. Substituted enyne undergoes cyclization to tetrahydropyridine in the presence of tris(2-furanyl)phosphinegold(I)chloride. Deprotection leads to the preparation of substituted pyridines, which could serve as intermediates in organic synthesis or as potential biologically active substances. Keywords: gold catalysis, enyne cyclization, pyridine derivatives
Pyridine sulphides as antituberculotic active compounds
Sýkora, Lukáš ; Klimešová, Věra (advisor) ; Kuneš, Jiří (referee)
This diploma thesis is devoted to antituberculosis drugs research. A very briefly depicts of genus Mycobacterium, structure and composition of mycobacterial cell wall allowed here better process and determination of mechanisms of antituberculosis drugs targets. The synthesis selected derivates of pyridine sulfides: 4- (phenethylsulfanyl)pyridine-2-carbonitriles are the main aim of the diploma thesis. As well as a possible mechanism of action these substances is discussed. Thus a series of 4-(phenethylsulfanyl)pyridine-2-carbonitriles were synthesized. The structures were confirmed by IR spectra, NMR spectra and elementary analyses. Antimycobacterial activities these compounds were tested against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. None of prepared substances exhibited activity (against M. tuberculosis) comparable to clinical used antituberculosis drugs. Significant activity was observed (in compare with isoniazide) against M. kansasii and M. avium.
Influence of the protective group on Au(I)-catalyzed cyclisation of 1,5-enynes
Charvát, Martin ; Pour, Milan (advisor) ; Klimešová, Věra (referee)
Within the framework of this Thesis, i have been occupied with optimalization of preparation in position 4 with phenyl substituted methyl ester of nicotinic acid, which was syntetized by gold catalyzed cycloizomerization of 1,5-enyne, which is not commercially available. This optimalized route of synthesis could be applied even for preparation in positions 2,3,4 and 6 substituted derivatives of pyridine.
Synthesis of Pyridazines by Ring Transformation Reaction
Budilová, Hana ; Klimešová, Věra (advisor) ; Pour, Milan (referee)
Charles University in Prague The Faculty of Pharmacy in Hradec Králové The Department of Inorganic and Organic Chemistry Candidate: Hana Budilová Supervisors: Doc. RNDr. Věra Klimešová, CSc. Prof. Dr. Rainer Beckert Title of Diploma Thesis: Synthesis of Pyridazines by Ring Transformation Reaction Pyridazines are heterocyclic compounds with two adjacent nitrogen atoms. There are a lot of synthetic approaches to get pyridazine. A number of specific transformations from other heterocyclic systems have been reported. This thesis deals with the synthesis of pyridazines by transformation of a four-membered heterocycle. Some new derivatives of 1-methyl-3-(4-tolylamino)-4-(4-tolylimino)-6-(4'- substituted-phenyl)-1,4-dihydropyridazines were synthesized by a ring transformation of four- membered 2 -1,2-diazetine. This compound was obtained by a cycloacylation reaction of methylhydrazine and bis-oxalimidoyl chloride. NMR and mass spectrometry confirmed structures of prepared compounds. 1-Methyl-3-(4-tolylamino)-4-(4-tolylimino)-6-phenyl-1,4-dihydropyridazine had been previously proven to possess antimycobacterial activity. The new derivatives were tested against Mycobacterium tuberculosis My 331/88, M. avium My 330/88, M. kansasii My 235/80 and M. kansasii 6 509/96. MIC values of these compounds range...
Heterocyclic Compounds with Antimycobacterial Activity
Herzigová, Petra ; Klimešová, Věra (advisor) ; Potáček, Milan (referee) ; Pytela, Oldřich (referee)
The dissertation thesis belongs to the conception of the research of potential antimycobacterial compounds. The aim of this work is synthesis of sulphide pyridine derivatives and the relationship between structure and antimycobacterial activity. Within the framework of this Thesis, the 112 substituted derivates of 4-(subst. fenylalkylsulfanyl)pyridine-2-carboxylic acid were synthesized. Antimycobacterial activity of prepared substances has been tested under in vitro conditions against M. tuberculosis, and non-tuberculous mycobacteria M. avium and M. kansasii. The series of 4-(subst. phenethylsulfanyl)pyridine-2-carbothioamide (MIC 1-32 µmol/L) represents the most active substances (MIC 1-32 µmol/L). These derivates don't reach the activity used antituberculosis drugs against M. tuberculosis, but their activities against M. avium exceed that of isoniazid. The synthesis of new structures as potential antimycobacterial compounds forms the second part of Thesis. All synthesis is based on the use of bis- arylimidoyl chlorides of oxalic acid of as starting material. None of prepared new compounds don't display an interesting antimycobacterial activity.
Optimization of the Synthesis of 3-(4-Bromophenyl)-5-hydroxymethyl-5,6-dihydro- pyran-2-one
Krenk, Ondřej ; Pour, Milan (advisor) ; Klimešová, Věra (referee)
Treatment of cancer still requires searching of new antineoplastics. Studies of biological activity of natural produkts show, that wide spektrum of biological aktivity have α,β- unsaturated-δ-laktons as potential substance with cytostatik aktivity. Goal of this work is optimalization of synthesis of 3-(4-bromfenyl)-5-hydroxymethyl-5,6-dihydro-2H-pyran-2-one as analogue of biologically active substance with potential cytostatic effect against cell line of colorectal carcinoma. Results obtained from this work can be employed in the development of simplier and more economical synthesis of potential biologically active analogues of α,β- unsaturated-δ-lactones.
Influence of the protective group on Au(I)-catalyzed cyclisation of 1,5-enynes
Charvát, Martin ; Pour, Milan (advisor) ; Klimešová, Věra (referee)
Within the framework of this Thesis, i have been occupied with optimalization of preparation in position 4 with phenyl substituted methyl ester of nicotinic acid, which was syntetized by gold catalyzed cycloizomerization of 1,5-enyne, which is not commercially available. This optimalized route of synthesis could be applied even for preparation in positions 2,3,4 and 6 substituted derivatives of pyridine.
Synthesis of tetrazoles as anticuberculotics
Vicherek, Petr ; Čonka, Patrik (advisor) ; Klimešová, Věra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Inorganic and Organic Chemistry Candidate: Petr Vicherek Supervisor: RNDr. Patrik Čonka, Ph.D. Title of diploma thesis: Synthesis of tetrazoles as antituberculotics Although significant progress in therapy of tuberculosis has been made since effective drugs were discovered in the second half of the 20th century, it is still widespread and refractory curable disease. The situation is complicated with growing appearance of resistant strains and for that reason it is necessary to search for new potential antituberculotics. The aim of this work was to continue with synthesis of antimycobacterial-efficient structures based on tetrazole. Firstly, we synthesised derivates of 1-aryl-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazole by the method of Williamson's synthesis, when the reaction of 1-aryl-1H-tetrazol-5-thiol with 3,5-dinitrobenzylchloride was performed. Conditions of the reactions were further optimalised. We prepared by the same way derivates of 1-fenyl-5-[(3,4,5- trimethoxybenzyl)sulfanyl]-1H-tetrazole afterwards, as analogues of previous tetrazoles missing the electron withdrawing 3,5-dinitrosubstitution. Furthermore, we concentrated on synthesis of substituted 1,5-diphenyl-1H-tetrazoles. Substituted...

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6 KLIMEŠOVÁ, Veronika
2 Klimešová, Vanda
6 Klimešová, Veronika
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