ISSN:0365-6233    

DOI:10.1002/ardp.19913240102

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractReinvestigation of the pigments ofPycnoporus sanguineus(Polyporaceae) yielded 4 new pigments of the 2‐amino‐phenoxazin‐3‐one type and the new phenoxazine ether pycnosanguin (9) besides cinnabarine (1). Unsubstituted phenoxazin‐3‐one was also shown among the pigments. Isolation and structure elucidation was performed after methylation of the crude acetone extract. The structures were established by spectral analysis and chemical degradations or inter

ISSN:0365-6233    

DOI:10.1002/ardp.19913240103

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractEs werden die 3‐Phenyl‐4‐amino‐3‐penten‐2‐on‐Derivate8a‐gaus dem Phenylaceton5über die 1, 3‐Diketone6a, bdargestellt. Die oxidative Cyclisierung von8bund9a,bgelingt mit Pb(OAc)4. Dadurch ist bewiesen, daß4bei derNenitzescu‐Reaktion durch Cyclisierung der intermediär gebildeten Chinolstufe3entstehen kann. Die Bildung eines intramolekularen CT‐Komplexes als Ursache für die Entstehung von4aus3bzw.

ISSN:0365-6233    

DOI:10.1002/ardp.19913240104

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractDie Umsetzung des α‐Hydroxymethylencyclopentanons2mit Acetylchinon1gibt die Spiroverbindung3. Aus α‐Hydroxymethylencyclohexanon7entstehen das Dibenzopyran8mit der Spiroverbindung9als Nebenprodukt. Die Verbindungen3, 8und9sind instabil, die Umlagerung zu6bzw.11wird NMR‐spektroskopisch verfolgt. Die Acetylierung von6und11führt zu5und12. Mit Salzsäure werden die Spiroverbindungen6und11zu16und17u

ISSN:0365-6233    

DOI:10.1002/ardp.19913240105

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractMethylation ofN‐substituted 1,2‐thiazetidine 1,1‐dioxides in the presence of lithium diisopropylamide (LDA) yields 4,4‐dimethyl derivatives. Monomethylation only occurs when one position at C‐4 is blocked by a silyl group, which, afterwards, can be removed by treatment with tetrabutylammonium fluoride (TBAF). A silyl protecting group at the nitrogen is easily removed by cleavage with TBAF on silica gel under mild c

ISSN:0365-6233    

DOI:10.1002/ardp.19913240106

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractThree novel series of pyrazolo[3,4‐b]quinolines were prepared, namely: 1‐(3‐substituted‐4‐phenylthiazolin‐2‐ylidene)hydrazinocarbonylmethyl‐1H‐pyrazolo[3,4‐b]quinolines3a‐d; 1‐(5‐substituted amino‐1,3,4‐thiadiazol‐2‐yl)methyl‐1H‐pyrazolo[3,4‐b]quinolines4b‐d, and 1‐(4‐substituted‐4H‐5‐thioxo‐1,2,4‐triazole‐3‐yl)methyl‐1H‐pyrazolo[3,4‐b]quinolines5a‐d. These compounds were prepared by cyclization of the new key intermediates 1‐(substituted thiocarbamoylhydrazinocarbonyl)methyl‐1H‐pyrazolo[3,4‐b]quinolines2a‐d. The alkylthio, aralkylthio6a‐fas well as theMannichbases8a‐fderived from compounds5a‐dwere also prepared. The structures of the new compounds were elucidated by elemental analyses, IR,1H‐NMR‐, and mass s

ISSN:0365-6233    

DOI:10.1002/ardp.19913240107

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractIm Rahmen einer intra‐arteriellen Chemotherapie von Patienten mit Lebermetastasen wurden die Blutspiegelverläufe von Mitomycin C (1) nach Verschluß der Arteria hepatica communis durch den Vasokonstriktor Glycylpressin (2) ermittelt. Der Gefäßverschluß mit2führt bei gleicher Dosierung im Gegensatz zu einer Bolusgabe von1ohne2zu signifikant (p<0.01) erniedrigten Blutspiegelwerten. Durch diese Verringerung der systematischen Verfügbarkeit um rund 50% wird die Verfügbarkeit im Tumorbereich entsprechend g

ISSN:0365-6233    

DOI:10.1002/ardp.19913240108

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractPschorrreaction of diazonium salt7in aqueous methanolic sulfuric acid afforded, besides lysicamine2, the orange colored sulfate of oxodibenzopyrrocoline (8). The structure is fully supported by an X‐ray analysis of its picrate salt. Selective ether cleavage of lysicamine (2) with 48% HBr afforded a hydrobromide of9, and free betaine9on treatment with pyridine‐water. Both compounds methylated on treatment with etherial diazomethane on nitrogen to give the known 2‐O N‐dimethylliriodendronine (11). Liriodendronine (10) was obtained from lysicamine (2) on heating with pyridine ·HBr at 189°C, and treatment with pyridine‐water, as a dark violet betaine. Betaine12was obtained by heating11·HCl to 200°C. The quaternary salts of lysicamine, lysicamine methiodide (3) and lysicamine methosulfate (4) were comparable in anticandidal activity to liriodenine (1), but were not as active as liriodenine me

ISSN:0365-6233    

DOI:10.1002/ardp.19913240109

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractCycloaddition reactions of the nitrilimines4—6withN‐arylmaleimides7and acrylamide (11) yield the pyrrolopyrazole derivatives8—10and 2‐pyrazolines12, respectively, in excellent yield. The regioselectivity and biological activities of some of the new compounds were inves

ISSN:0365-6233    

DOI:10.1002/ardp.19913240110

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY

摘要:

AbstractA series ofpara‐substituted triamterene derivatives (Table 1) were evaluated for their antiarrhythmic propertiesin vitro. Pharmacological evaluation of the compounds and some class‐I‐ (quinidine, lidocaine, and propafenone) as well as class‐III‐antiarrhythmic drugs (±)‐sotalol and amiodarone was carried out by measuring the functional refractory period (FRP), the maximal driving frequency (MDF) and the force of myocardial contractions (FC) of electrically stimulated guinea pig atria. The increase in FRP and the decrease in MDF was most pronounced with the class‐I‐antiarrhythmic drugs, but these compounds showed the typical negative inotropic effects, too. For the class‐III‐antiarrhythmics only a weak influence on FRP and MDF could be demonstrated, while FC was not altered in the presence of (±)‐sotalol and amiodarone. Neutral substituted triamterenes like compounds2—5as well as most of the benzyltriamterene derivatives showed similar or stronger effects on FRP and MDF as (±)‐sotalol and amiodarone. With the exception of4and5, these effects were combined with an increase of FC. Compounds6and7, well known potent diuretics, showed no influence to FRP, MDF and FC. Therefore, we conclude different mechanisms for the antikal

ISSN:0365-6233    

DOI:10.1002/ardp.19913240111

出版商:WILEY‐VCH Verlag    

年代:1991

数据来源: WILEY