ACETATES Dotaz Zobrazit nápovědu
Concise international chemical assessment document, ISSN 1020-6167 64
iv, 49 s. : tab. ; 30 cm
- MeSH
- acetáty škodlivé účinky toxicita MeSH
- bezpečnost MeSH
- hodnocení rizik MeSH
- vystavení vlivu životního prostředí MeSH
- Konspekt
- Organická chemie
- NLK Obory
- chemie, klinická chemie
- NLK Publikační typ
- publikace WHO
A panel of lipases was screened for the selective acetylation and alcoholysis of silychristin and silychristin peracetate, respectively. Acetylation at primary alcoholic group (C-22) of silychristin was accomplished by lipase PS (Pseudomonas cepacia) immobilized on diatomite using vinyl acetate as an acetyl donor, whereas selective deacetylation of 22-O-acetyl silychristin was accomplished by Novozym 435 in methyl tert-butyl ether/ n-butanol. Both of these reactions occurred without diastereomeric discrimination of silychristin A and B. Both of these enzymes were found to be capable to regioselective deacetylation of hexaacetyl silychristin to afford penta-, tetra- and tri-acetyl derivatives, which could be obtained as pure synthons for further selective modifications of the parent molecule.
- MeSH
- acetáty chemická syntéza MeSH
- acetylace MeSH
- bakteriální proteiny metabolismus MeSH
- biokatalýza MeSH
- Burkholderia cepacia enzymologie MeSH
- enzymy imobilizované metabolismus MeSH
- lipasa metabolismus MeSH
- molekulární struktura MeSH
- registrace MeSH
- silymarin chemie MeSH
- stereoizomerie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
A new series of salicylanilide acetates was synthesized and evaluated for their in vitro antifungal and antituberculotic activity. Some of the evaluated compounds possessed comparable or better antifungal activity than a fluconazole standard. All these compounds exhibited very good potential and their in vitro activity against drug resistant and sensitive clinical isolates of Mycobacteria were found to be equivalent or better than a standard of isoniazide, a well-known first-line drug for tuberculosis treatment.
- MeSH
- antibakteriální látky farmakologie chemická syntéza chemie MeSH
- antifungální látky farmakologie chemická syntéza chemie MeSH
- buněčné linie MeSH
- Candida albicans účinky léků MeSH
- flukonazol farmakologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- mikrobiální viabilita účinky léků MeSH
- molekulární struktura MeSH
- Mycobacterium účinky léků MeSH
- salicylanilidy farmakologie chemická syntéza chemie MeSH
- viabilita buněk účinky léků MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
4th ed. Nestr.
- Konspekt
- Patologie. Klinická medicína
- NLK Obory
- alergologie a imunologie
Environmental health criteria ; 115
126 s. : 1 obr., 9 tab., bibliogr.
- Klíčová slova
- ethylenglykol, charakteristika, účinky nepříznivé, vliv na zdraví, toxicita, octany - prostředí životní - znečišťování - účinky - materiály WHO,
- Konspekt
- Lékařské vědy. Lékařství
- NLK Obory
- environmentální vědy
- toxikologie
- NLK Publikační typ
- publikace WHO
A novel approach to the synthesis of (purin-6-yl)acetates was developed based on Pd-catalyzed cross-coupling reactions of 6-chloropurines with a Reformatsky reagent. Their reduction with NaBH4 and treatment with MnO2 gave 6-(2-hydroxyethyl)purines, while reactions with amines in presence of NaCN afforded 6-(carbamoylmethyl)purines. Mesylation of the 6-(2-hydroxyethyl)purines followed by nucleophilic substitutions gave rise to several 6-(2-substituted ethyl)purines. This methodology was successfully applied to the synthesis of substituted purine bases and nucleosides for cytostatic and antiviral activity screening. None of the compounds exerted significant activity.
