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Synthesis of potent neuroprotective butenolides based on plant smoke derived 3,4,5-Trimethylfuran-2(5H)-one and 3-methyl-2H-furo[2,3-c]pyrone-2-one
D. Naidoo, M. Pošta, A. Roy, M. Kulkarni, J. Van Staden,
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc19034608
- MeSH
- acetylcholinesterasa metabolismus MeSH
- depresivní poruchy farmakoterapie MeSH
- furany chemická syntéza chemie farmakologie MeSH
- gama-butyrolakton analogy a deriváty chemická syntéza chemie farmakologie MeSH
- inhibitory MAO chemická syntéza chemie farmakologie MeSH
- lidé MeSH
- molekulární struktura MeSH
- monoaminoxidasa metabolismus MeSH
- neurodegenerativní nemoci farmakoterapie MeSH
- neuroprotektivní látky chemická syntéza chemie farmakologie MeSH
- pyrany chemická syntéza chemie farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Smoke derived karrikinolide and trimethylbutenolide exerted neuroprotective effects against monoamine oxidase and acetylcholinesterase. Synthesis of potent analogs was achieved. Sulphur substitution in the bicyclic ring structure of KAR1 displayed the most encouraging activity returning IC50 values of 13.75 ± 0.001 μM and 0.03 ± 0.02 μM for monoamine oxidase A and B and 0.08 ± 0.006 μM for acetylcholinesterase. Neuroprotective butenolides may be particularly useful in the treatment of depressive disorders, Alzheimer's and Parkinson's diseases.
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- $a 10.1016/j.phytochem.2019.03.014 $2 doi
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- $a Naidoo, Devashan $u Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal Pietermaritzburg, Private Bag X01, Scottsville, 3209, South Africa.
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- $a Synthesis of potent neuroprotective butenolides based on plant smoke derived 3,4,5-Trimethylfuran-2(5H)-one and 3-methyl-2H-furo[2,3-c]pyrone-2-one / $c D. Naidoo, M. Pošta, A. Roy, M. Kulkarni, J. Van Staden,
- 520 9_
- $a Smoke derived karrikinolide and trimethylbutenolide exerted neuroprotective effects against monoamine oxidase and acetylcholinesterase. Synthesis of potent analogs was achieved. Sulphur substitution in the bicyclic ring structure of KAR1 displayed the most encouraging activity returning IC50 values of 13.75 ± 0.001 μM and 0.03 ± 0.02 μM for monoamine oxidase A and B and 0.08 ± 0.006 μM for acetylcholinesterase. Neuroprotective butenolides may be particularly useful in the treatment of depressive disorders, Alzheimer's and Parkinson's diseases.
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- $a gama-butyrolakton $x analogy a deriváty $x chemická syntéza $x chemie $x farmakologie $7 D015107
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- $a acetylcholinesterasa $x metabolismus $7 D000110
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- $a depresivní poruchy $x farmakoterapie $7 D003866
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- $a vztah mezi dávkou a účinkem léčiva $7 D004305
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- $a furany $x chemická syntéza $x chemie $x farmakologie $7 D005663
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- $a Pošta, Martin $u Institute of Organic Chemistry and Biochemistry AS CR, v.v.i., Flemingovonám. 2, 16610, Prague 6, Czech Republic.
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- $a Roy, Ayan $u Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal Pietermaritzburg, Private Bag X01, Scottsville, 3209, South Africa.
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- $a Kulkarni, Manoj $u Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal Pietermaritzburg, Private Bag X01, Scottsville, 3209, South Africa.
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- $a Van Staden, Johannes $u Research Centre for Plant Growth and Development, School of Life Sciences, University of KwaZulu-Natal Pietermaritzburg, Private Bag X01, Scottsville, 3209, South Africa. Electronic address: rcpgd@ukzn.ac.za.
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- $w MED00003829 $t Phytochemistry $x 1873-3700 $g Roč. 163, č. - (2019), s. 187-194
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