Twelve positional isomers of diamino pseudodisaccharide derivatives with gluco-gluco configuration have been prepared using aziridine-ring cleavage of epimino derivatives of 1,6-anhydro-beta-D-hexopyranoses of the D-allo, D-manno, and D-galacto configuration by 2-, 3-, and 4-amino derivatives of 1,6-anhydro-beta-D-glucopyranose. The N-substitution of the aziridine ring by a 2-nitrobenzenesulfonyl group and ionic-liquid solvent (N-methylpyridinium tosylate) was used to obtain cleavage products in high yield (64-93%). The cleavage reactions proceeded according to the Fürst-Plattner rule and only trans-diaxial stereoisomers were formed.

• MeSH
• aminocukry chemická syntéza   chemie   MeSH
• aziridiny chemie   MeSH
• galaktosa analogy a deriváty   chemie   MeSH
• glukosa analogy a deriváty   chemie   MeSH
• hexosy chemie   MeSH
• konformace sacharidů MeSH
• magnetická rezonanční spektroskopie MeSH
• mannosa analogy a deriváty   chemie   MeSH
• molekulární struktura MeSH
• sacharidové sekvence MeSH
• stereoizomerie MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• 1,6-anhydro-beta-glucopyranose MeSH Prohlížeč
• aminocukry MeSH
• aziridine MeSH Prohlížeč
• aziridiny MeSH
• galactosan MeSH Prohlížeč
• galaktosa MeSH
• glukosa MeSH
• hexosy MeSH
• mannosa MeSH
• mannosan MeSH Prohlížeč

Convulsive activity of N-(3,5-dimethoxy-4-propoxy-phenyl-ethyl)-aziridine (FAZ-4), a newly synthetized aziridine compound was studied in rats. There is a lack of tonic component of major paroxysm in comparison with the classical convulsive agent pentylenetetrazol. This effect of FAZ-4 is probably due to the forebrain mechanism without the midbrain involvement. Both anticonvulsants tested suppressed seizures in a different manner, however triazolam exerted stronger anticonvulsive activity than the same dose of diazepam did.

• MeSH
• antikonvulziva farmakologie   MeSH
• aziridiny farmakologie   MeSH
• diazepam farmakologie   MeSH
• krysa rodu Rattus MeSH
• potkani Wistar MeSH
• triazolam farmakologie   MeSH
• záchvaty chemicky indukované   patofyziologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• antikonvulziva MeSH
• aziridiny MeSH
• diazepam MeSH
• N-((3,5-dimethoxy-4-propoxyphenyl)ethyl)aziridine MeSH Prohlížeč
• triazolam MeSH

• MeSH
• aziridiny farmakologie   MeSH
• krysa rodu Rattus MeSH
• pohybová aktivita účinky léků   MeSH
• učení vyhýbat se účinky léků   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aziridiny MeSH
• N-(3,4,5-trimethoxyphenylethyl)aziridine MeSH Prohlížeč

• MeSH
• aziridiny farmakologie   MeSH
• cholinesterasové inhibitory farmakologie   MeSH
• cholinesterasy krev   metabolismus   MeSH
• kinetika MeSH
• krysa rodu Rattus MeSH
• lidé MeSH
• meskalin metabolismus   MeSH
• mozek účinky léků   enzymologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aziridiny MeSH
• cholinesterasové inhibitory MeSH
• cholinesterasy MeSH
• meskalin MeSH
• N-(3,4,5-trimethoxyphenylethyl)aziridine MeSH Prohlížeč

Dinosylated α-d-glucopyranoside was directly transformed into α-d-altropyranosides via in situ formed N-4-nosyl Hough-Richardson aziridine with nitrogen nucleophiles under mild conditions in fair to excellent yields. The scope of the aziridine ring-opening reaction was substantially broadened contrary to the conventional methods introducing solely the azide anion at high temperatures. If necessary, the N-4-nosyl Hough-Richardson aziridine can be isolated by filtration in a very good yield and high purity.

• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH

The central effect of mescaline and of its derivative N-[3,4,5- trimethoxyphenylethyl]-aziridine (FAZ) after their stereotaxic administration into the lateral ventricle of the brain was studied in behavioural experiments on rats. The effect of the two substances was tested by a method studying memory elicitation in response to appetitive motivation in a multiple T-maze. The results show that both substances worsened the behaviour in question. The negative effect of mescaline (lengthening of the time of passage through the maze) was manifested both immediately and several weeks after a single dose. FAZ likewise worsened the test reaction, but its effect was less pronounced than that of mescaline.

• MeSH
• aziridiny aplikace a dávkování   farmakologie   MeSH
• chování zvířat účinky léků   MeSH
• inbrední kmeny potkanů MeSH
• injekce intraventrikulární MeSH
• krysa rodu Rattus MeSH
• meskalin aplikace a dávkování   analogy a deriváty   farmakologie   MeSH
• orientace účinky léků   MeSH
• paměť účinky léků   MeSH
• prostorové chování * MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Názvy látek
• aziridiny MeSH
• meskalin MeSH

Naturally occurring oligoamines, such as spermine, spermidine, and putrescine, are well-known regulators of gene expression. These oligoamines frequently have short alkyl spacers with varying lengths between the amines. Linear polyethylenimine (PEI) is a polyamine that has been widely applied as a gene vector, with various formulations currently in clinical trials. In order to emulate natural oligoamine gene regulators, linear random copolymers containing both PEI and polypropylenimine (PPI) repeat units were designed as novel gene delivery agents. In general, statistical copolymerization of 2-oxazolines and 2-oxazines leads to the formation of gradient copolymers. In this study, however, we describe for the first time the synthesis of near-ideal random 2-oxazoline/2-oxazine copolymers through careful tuning of the monomer structures and reactivity as well as polymerization conditions. These copolymers were then transformed into near-random PEI-PPI copolymers by controlled side-chain hydrolysis. The prepared PEI-PPI copolymers formed stable polyplexes with GFP-encoding plasmid DNA, as validated by dynamic light scattering. Furthermore, the cytotoxicity and transfection efficiency of polyplexes were evaluated in C2C12 mouse myoblasts. While the polymer chain length did not significantly increase the toxicity, a higher PPI content was associated with increased toxicity and also lowered the amount of polymers needed to achieve efficient transfection. The transfection efficiency was significantly influenced by the degree of polymerization of PEI-PPI, whereby longer polymers resulted in more transfected cells. Copolymers with 60% or lower PPI content exhibited a good balance between high plasmid-DNA transfection efficiency and low toxicity. Interestingly, these novel PEI-PPI copolymers revealed exceptional serum tolerance, whereby transfection efficiencies of up to 53% of transfected cells were achieved even under 50% serum conditions. These copolymers, especially PEI-PPI with DP500 and a 1:1 PEI/PPI ratio, were identified as promising transfection agents for plasmid DNA.

• MeSH
• aziridiny MeSH
• DNA * chemie   MeSH
• myši MeSH
• plazmidy genetika   MeSH
• polyethylenimin chemie   MeSH
• polymery * chemie   MeSH
• technika přenosu genů MeSH
• transfekce MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• aziridine MeSH Prohlížeč
• aziridiny MeSH
• DNA * MeSH
• polyethylenimin MeSH
• polymery * MeSH

• MeSH
• alely * MeSH
• aziridiny toxicita   MeSH
• aziriny toxicita   MeSH
• druhová specificita MeSH
• hlavní histokompatibilní komplex * MeSH
• inbrední kmeny potkanů MeSH
• krysa rodu Rattus MeSH
• mutace * MeSH
• syndrom MeSH
• těhotenství MeSH
• teratogeny * MeSH
• zadní končetina abnormality   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• těhotenství MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Názvy látek
• aziridine MeSH Prohlížeč
• aziridiny MeSH
• aziriny MeSH
• teratogeny * MeSH

Effect of two anticonvulsants with different mechanism of action, i.e. alprazolam and ketamine, was tested in two types of seizure activity. The first one was induced by N-(3,5-dimethoxy-4-propoxyphenylethyl)-aziridine, the second one by pentylenetetrazol. While alprazolam alleviated both the minimal as well as major paroxysms, ketamine suppressed only major seizures. These effects are discussed in terms of the both N-methyl-D-aspartate and GABA receptors involvement.

• MeSH
• alprazolam terapeutické užití   MeSH
• antikonvulziva terapeutické užití   MeSH
• aziridiny MeSH
• ketamin terapeutické užití   MeSH
• konvulzíva MeSH
• krysa rodu Rattus MeSH
• pentylentetrazol MeSH
• potkani Wistar MeSH
• záchvaty chemicky indukované   farmakoterapie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• alprazolam MeSH
• antikonvulziva MeSH
• aziridiny MeSH
• ketamin MeSH
• konvulzíva MeSH
• N-((3,5-dimethoxy-4-propoxyphenyl)ethyl)aziridine MeSH Prohlížeč
• pentylentetrazol MeSH

• MeSH
• aziridiny chemická syntéza   chemie   MeSH
• isomerie MeSH
• konformace sacharidů MeSH
• molekulární struktura MeSH
• oxidace-redukce MeSH
• sacharidy chemická syntéza   chemie   MeSH
• stereoizomerie MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• aziridiny MeSH
• sacharidy MeSH