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Synthesis of substituted arylguanidines as potential drugs IX.
Vidrna, Ondřej ; Palát, Karel (advisor) ; Špulák, Marcel (referee)
Charles university in Prague Faculty of Pharmacy in Hradec Králové Department of Anorganic and Organic Chemistry Candidate: Ondřej Vidrna Supervisor: PharmDr. Karel Palát, CSc Title of diploma thesis: Synthesis of substituted arylguanidines as potential drugs IX. The increasing incidence of diseases caused by fungal and mycotic pathogens, many of which acquire resistance to available antifungal substances, causes the need for a search for new molecules inhibiting their growth. The worldwide research is focused on substances derived from guanidine which were found to be potentially active against many strains of fungi and bacteria. Faculty of Pharmacy in Hradec Králové has been researching these substances for many years. The aim is to get the most active compounds from the group of substituted arylguanidines and find a structure-activity relationships effect of these substances. In this study the seven previously undescribed molecules were synthesized: 1-(4- methyl-2-octylsulfanyl)phenylguanidinium nitrate, 1-(4-methyl-2-dodecylsulfanyl) phenylguanidinium nitrate, 1-(4-methyl-2-dodecylsulfanyl)phenyl-3,3-dimethylguanidine, octyl-(4-methyl-2-nitrophenyl)sulfide, 5-methyl-2-(octylsulfanyl)aniline, dodecyl-(4-methyl-2- nitrophenyl)sulfide and 5-methyl-2-(dodecylsulfanyl)aniline. Three of them were...
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Synthesis of substituted arylguanidines as potential drugs VII.
Bromand, Nasir ; Palát, Karel (advisor) ; Macháček, Miloš (referee)
Pathological fungi carry the ability to cause serious medical problems and moreover cause various diseases. Drug therapy and new active compounds against these medical problems are still being researched. The long-term objective is to uncover the active compounds at the Faculty of Pharmacy, Charles University. In our study, we synthesized 3-(4-bromophenyl)-1,1-diethylguanidine, and 2 novel compounds: 3-(4- dodecylsulfanylphenyl)-1,1-diethylguanidine and 3-(3-bromophenyl)-1,1- diethylguanidine. We also studied the oxidation of 1-(4- tetradecylsulfanylphenyl)guanidinium nitrate, thus, making it the third novel compound 1-(4-tetradecylsulfonylphenyl)guanidinium nitrate we synthesized.
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Synthesis of substituted arylguanidines as potential drugs IX.
Vidrna, Ondřej ; Palát, Karel (advisor) ; Špulák, Marcel (referee)
Charles university in Prague Faculty of Pharmacy in Hradec Králové Department of Anorganic and Organic Chemistry Candidate: Ondřej Vidrna Supervisor: PharmDr. Karel Palát, CSc Title of diploma thesis: Synthesis of substituted arylguanidines as potential drugs IX. The increasing incidence of diseases caused by fungal and mycotic pathogens, many of which acquire resistance to available antifungal substances, causes the need for a search for new molecules inhibiting their growth. The worldwide research is focused on substances derived from guanidine which were found to be potentially active against many strains of fungi and bacteria. Faculty of Pharmacy in Hradec Králové has been researching these substances for many years. The aim is to get the most active compounds from the group of substituted arylguanidines and find a structure-activity relationships effect of these substances. In this study the seven previously undescribed molecules were synthesized: 1-(4- methyl-2-octylsulfanyl)phenylguanidinium nitrate, 1-(4-methyl-2-dodecylsulfanyl) phenylguanidinium nitrate, 1-(4-methyl-2-dodecylsulfanyl)phenyl-3,3-dimethylguanidine, octyl-(4-methyl-2-nitrophenyl)sulfide, 5-methyl-2-(octylsulfanyl)aniline, dodecyl-(4-methyl-2- nitrophenyl)sulfide and 5-methyl-2-(dodecylsulfanyl)aniline. Three of them were...
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Synthesis of substituted arylguanidines as potential drugs XI.
Swedi, Firdaus Shaban ; Palát, Karel (advisor) ; Macháček, Miloš (referee)
This study focus on synthesis of novel compounds as potential agents for the therapy of mycoses. The following four novel compounds were synthesized: 1-(4-(octylsulfanyl)-3-(trifluoromethyl)phenyl)guanidine, 1,1-dimethyl-3-(4-(octylsulfanyl)-3-(trifluoromethyl)phenyl)guanidine, 1-(4-(decylsulfanyl)-3-(trifluoromethyl)phenylguanidine, 3-(4-(decylsulfanyl)-3-(trifluoromethyl)phenyl-1,1-dimethylguanidine. All intermediary and final crystalline products formed were thoroughly purified and characterized by Thin Layer Chromatography (TLC) and Melting points. Structures were elucidated on the basis of Infrared (IR) and Nuclear Magnetic Resonance (NMR) spectroscopy. 1- (4-(octylsulfanyl)-3-(trifluoromethyl)phenyl)guanidine was evaluated for in vitro antimicrobial activity on different fungal and bacterial strains.
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Synthesis of substituted arylguanidines as potential drugs VII.
Bromand, Nasir ; Palát, Karel (advisor) ; Macháček, Miloš (referee)
Pathological fungi carry the ability to cause serious medical problems and moreover cause various diseases. Drug therapy and new active compounds against these medical problems are still being researched. The long-term objective is to uncover the active compounds at the Faculty of Pharmacy, Charles University. In our study, we synthesized 3-(4-bromophenyl)-1,1-diethylguanidine, and 2 novel compounds: 3-(4- dodecylsulfanylphenyl)-1,1-diethylguanidine and 3-(3-bromophenyl)-1,1- diethylguanidine. We also studied the oxidation of 1-(4- tetradecylsulfanylphenyl)guanidinium nitrate, thus, making it the third novel compound 1-(4-tetradecylsulfonylphenyl)guanidinium nitrate we synthesized.
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