摘要:

AbstractDie Synthese der Titelverbindungen vom Typ5bzw.7aus den Aldehyden2bzw.6a,bund den primär/tertiären Nitroketenaminalen1c,d,ewird beschrieben. Mit dem primär/sekundären Nitroketenaminal1bund2erhält man ein 1,4‐Dihydropyri

ISSN:0365-6233    

DOI:10.1002/ardp.19933260103

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractTerephthalic acid at 20 mg/kg/day in lowered serum cholesterol and triglyceride levels in rats. The cholesterol content was lowered in the lipoprotein fractions. The effects of the agents onde novolipid synthesis showed that similar enzymes were affected in rat liver and small intestinal mucosa cells as when compared toin vitrotissue culture cells from rats and humans,e.g. reduction of acyl CoA cholesterol acyl transferase and elevation of neutral cholesterol ester hydrolase activities suggest that net cholesterol esters deposition in foam cells should be reduced and plaque growth should be slowed. The suppression of LDL receptor binding and degradation by the drug suggest that less apoB lipoproteins are taken up by peripheral tissues. The elevated HDL receptor binding and internalization in the liver suggest that the drug accelerates cholesterol return to the liver. Additional studies show that cholesterol and bile acid secretion in the bile is elevated. However, the bile acids secreted are not lithogenic. Acute toxicity studies show that the agent appears to be safe in rodents. Two observations of increased serum alkaline phosphophatase levels and increased liver vacuolation suggest some alteration of hepatic cell morphology, which requires further investigation.

ISSN:0365-6233    

DOI:10.1002/ardp.19933260104

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

Abstract2‐Furoic acid was shown to be effective in lowering both serum cholesterol and serum triglyceride levels significantly in rats with an elevation of HDL cholesterol level at 20 mg/kg/day orally. LDL receptor activity was reduced in hepatocytes, aorta foam cells, small intestinal epithelium cells and fibroblasts. HDL receptor activity was elevated in the rat hepatocytes and small intestinal cells. These activities were correlated with inhibition of acyl CoA cholesterol acyl transferase activity. Neutral cholesterol ester hydrolase activity was elevated in rat hepatocytes and human fibroblasts. Thus, 2‐furoic acid appears to interfere directly with activity of intracellular enzymes rather than affecting high affinity‐mediated lipoprotein membrane receptors.In vivotreatment with 2‐furoic acid led to reduction in the liver and small intestine ATP dependent citrate lyase, acetyl CoA synthetase, acyl CoA cholesterol acyl transferase,sn‐glycerol 3‐phosphate acyl transferase, phosphatidylate phosphohydrolase and heparin induced lipoprotein lipase activities.2‐Furoic acid reduced biliary cholesterol levels but the agent increased bile salts which are lithogenic. Acute toxicity studies in mice suggest that the agent has some hepatic toxicity effects. The LD50was relatively low at 250 mg/

ISSN:0365-6233    

DOI:10.1002/ardp.19933260105

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractDuring investigations on theN‐oxygenation of adenine (1) the enzymatic formation of adenine 1‐N‐oxide3was demonstrated for the first time. The identity of this metabolite was confirmed by its chromatographic behaviour and UV‐spectrum recorded after HPLC separation. Adenine 1‐N‐oxide (3) and similar oxygenated derivatives of adenine were synthesized as reference substances. The enzymatic formation of3exhibits the typical characteristics of a reaction catalysed by microsomal mono‐oxygenases. In induction experiments, an increase in the rate of formation of3after pretreatment with phenobarbital was observed. A participation of those isoenzymes of the cytochrome P‐450 enzyme system which can be induced by phenobarb

ISSN:0365-6233    

DOI:10.1002/ardp.19933260106

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractWir beschreiben [4+2]‐Cycloadditionen von Azulen (2) und 1‐Nitroazulen (14) mit dem extrem elektronenarmen, s‐cis‐fixierten Diazadiensystem von 3,6‐Bis(triflluormethyl)‐1,2,4,5‐tetrazin (1). In Ergänzung früherer Befunde reagiert1mit2vermutlich nach einerzweistufigen[4+2]‐Cycloaddition über das zwitterionische8und10zum Benzo[f]phthalazin5, über8und9zum Azuleno[d]pyridazin3und dem Azin4. Die Umsetzung von1mit 1‐Nitroazulen (14) liefert in mäßiger Ausbeute die Azuleno[d]pyridazine3und19als einz

ISSN:0365-6233    

DOI:10.1002/ardp.19933260107

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThe synthesis of all the four stereomers of the alkaloid woodinine (12a)1)is described and the stereochemical conclusions ofPaïs3)andStill6)are discussed. The absol. configurations of woodinine (12a) and its diastereomer8bare unequivocally deduced from the pertinent piperazinediones16and17

ISSN:0365-6233    

DOI:10.1002/ardp.19933260108

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThe coupling of 1‐amino‐2,6,6‐tricyanocyclohexadiene derivatives1‐3with a variety of aryldiazonium salts produces the hydrazones5‐7which in the presence of weak base in ethanol at elevated temperature furnish 2‐aryl‐4‐cyanopyridazin‐3(2H)‐ones8‐10. In boiling toluene, however, the tautomeric hydrazones

ISSN:0365-6233    

DOI:10.1002/ardp.19933260109

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractAus den 1‐13C‐markierten 4‐monosubstituierten Benzilen1a‐cwurden mit den Harnstoffen3a‐d5‐Aryl‐5‐phenylhydantoine6a‐cbzw. 3‐substituierte 5‐Aryl‐5‐phenylhydantoine9a‐ials Isotopomerengemische dargestellt. Massen‐ und13C‐NMR‐spektrometrisch wird die Verteilung der13C‐Markierung auf C‐4 und C‐5 ermittelt. Wie bei der Benzilsäureumlagerung wandert auch hier der 4‐Methyl‐ bzw. 4‐Methoxyphenylrest weniger leicht als der unsubstituierte Phenylrest und dieser weniger leicht als der 4‐Chlorphenylrest. Der Unterschied zwischen Phenyl‐ und 4‐Chlorphenylrest ist allerdings nur klein und kehrt sich in einem Fall sogar geringfügig um. Der Einfluß der Substituenten auf die Richtung der Umlagerung wird mit einer thermodynamischen Steuerung der Reaktion durch vo

ISSN:0365-6233    

DOI:10.1002/ardp.19933260110

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

Abstract„γ‐Lactonisierte”︁ Neuroleptika (1,2a‐c) können aus den α‐Formyl‐, α‐Carboxy‐ und α‐Methylenlactonen5‐7a,bdurch Umsetzen mit den Aminen8a‐cerhalten werden.6aund1a‐cfielen alscis/trans‐Gemische mit über‐wiegendercis‐Form,6bund2aalscis/trans‐Gemische mit überwiegendertrans‐Form an.

ISSN:0365-6233    

DOI:10.1002/ardp.19933260111

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractBei der Reaktion der Dithionmalonester1mit den Formamidacetalen2entsteht ein Gemisch der 2‐(Dialkylaminomethylen)dithionmalonester4und der Thionacrylester6. Die Kondensation von4mit Hydrazinen liefert die Pyrazole7und8, mit Hydroxylaminsulfonsäure die Isothiazole10und mit Amidinen die Pyrimidine11

ISSN:0365-6233    

DOI:10.1002/ardp.19933260112

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY