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| Description
| - Starting from three monomeric ergolines (terguride 1, festuclavine 2, pergolide 3) N,N'-spacer-linked oligomeric derivatives were prepared using different aliphatic or arylalkyl spacers. The compounds have been evaluated for their in vitro antiplasmodial activity against the chloroquine-sensitive strain poW and the chloroquine-resistant clone Dd2 of Plasmodium falciparum. Additionally, the cytotoxic effects against mouse fibroblasts (NIH 3T3) in vitro, and human hepatocytes were evaluated. All monomers displayed only a weak antiplasmodial effect, but N-1,N-1'-spacer-linked dimerization substantially enhanced their antiplasmodial activity. The best activities were observed for compounds showing a distance of six carbon atoms between two monomers, which can be obtained by aliphatic or p-xylene linkers. The N-6,N-6'-spacer-linked depropylpergolide dimer 3i exhibited the highest antiplasmodial activity of all compounds tested (IC50 values: 0.14 and 0.13 M against poW and Dd2, respectively). Unfortunately,
- Starting from three monomeric ergolines (terguride 1, festuclavine 2, pergolide 3) N,N'-spacer-linked oligomeric derivatives were prepared using different aliphatic or arylalkyl spacers. The compounds have been evaluated for their in vitro antiplasmodial activity against the chloroquine-sensitive strain poW and the chloroquine-resistant clone Dd2 of Plasmodium falciparum. Additionally, the cytotoxic effects against mouse fibroblasts (NIH 3T3) in vitro, and human hepatocytes were evaluated. All monomers displayed only a weak antiplasmodial effect, but N-1,N-1'-spacer-linked dimerization substantially enhanced their antiplasmodial activity. The best activities were observed for compounds showing a distance of six carbon atoms between two monomers, which can be obtained by aliphatic or p-xylene linkers. The N-6,N-6'-spacer-linked depropylpergolide dimer 3i exhibited the highest antiplasmodial activity of all compounds tested (IC50 values: 0.14 and 0.13 M against poW and Dd2, respectively). Unfortunately, (en)
- Z monomerních ergolinů (terguride 1, festuclavin 2, pergolid 3) byly připraveny oligomerní deriváty za použití různých alifatických a arylalkylových spojek. U připravených sloučenin byly studovány antiplasmodiální účinky proti chlorochin-sensitivnímu kmenu poW a chlorochin-resistentnímu klonu Dd2 Plasmodium falciparum. Dále byla studována cytotoxicita na myších fibroblastech (NIH 3T3) a na lidských hepatocytech in vitro. Všechny monomery vykazovaly pouze slabý účinek, ale dimerizace zvyšovala antiplasmodiální aktivitu. Nejlepší účinek byl pozorován u sloučenin s 6 uhlíkovou vzdáleností mezi dvěma monomery. N-6,N-6' depropylpergolidový dimer (3i) vykazoval nejvyšší antiplasmodiální aktivitu ze všech testovaných látek (IC50 0,14 pro poW a 0,13 pro Dd2), ale vykazoval toxicitu na myších fibroblastech (IC50 0,1) a na lidských hepatocytech. Naproti tomu trimer festuclavinu (2f) a tetramer terguridu (1g) vykazoval antiplasmodiální aktivitu bez toxicity. (cs)
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| Title
| - In vitro antiplasmodial activities of semisynthetic N,N'-spacer-linked oligomeric ergolines
- In vitro antiplasmodial activities of semisynthetic N,N'-spacer-linked oligomeric ergolines (en)
- In vitro antiplasmodiální aktivity semisyntetických N,N'-oligomerních ergolinů (cs)
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| skos:prefLabel
| - In vitro antiplasmodial activities of semisynthetic N,N'-spacer-linked oligomeric ergolines
- In vitro antiplasmodial activities of semisynthetic N,N'-spacer-linked oligomeric ergolines (en)
- In vitro antiplasmodiální aktivity semisyntetických N,N'-oligomerních ergolinů (cs)
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| skos:notation
| - RIV/61989592:15110/04:00000806!RIV/2005/MSM/151105/N
|
| http://linked.open.../vavai/riv/strany
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
| - P(IAA4020901), Z(AV0Z5020903), Z(MSM 151100003)
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
| |
| http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15110/04:00000806
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - Malaria;toxicity;ergot alkaloids;supramolecular chemistry (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Bioorganic & Medicinal Chemistry
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| http://linked.open...in/vavai/riv/obor
| |
| http://linked.open...ichTvurcuVysledku
| |
| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...vavai/riv/projekt
| |
| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Křen, Vladimír
- Ulrichová, Jitka
- Fišerová, Anna
- Kuzma, M.
- Bienzle, Ulrich
- Eich, Eckart
- Jenett-Siems, Kristina
- Kraft, Carola
- Köhler, Inga
- Pertz, Heinz
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| http://linked.open...n/vavai/riv/zamer
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| issn
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| number of pages
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| http://localhost/t...ganizacniJednotka
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