摘要:

AbstractAlkylation of the 3‐chloroethyl substituted β‐sultam1with bromoacetates yields theN‐ and 3‐substituted β‐sultams2; exchange of halogens affords esters3. Reactions of1or of the analogues8with isocyanates make the carbamoyl derivatives5,6, and9available. While cyclization of6withn‐BuLi in the presence of HMPT yields the bicyclic β‐sultams7, the analogous reaction of9failed. The bicyclic β‐sultams12and14are obtained from 3‐hydroxyalkyl β‐sultams11and13and carbonyl compounds. None of the prepared β‐sultams showed

ISSN:0365-6233    

DOI:10.1002/ardp.19933260802

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThermisch induzierte intramolekulare [3 + 2]‐Cycloadditionsreaktionen der Nicotinium‐dicanmethylide4a‐c, die am Pyrrolidinstickstoff mit verschieden langen ω‐Alkinseitenketten substituiert sind, führen in guten Ausbeuten zu entspr. neuen, heterocyclisch anellierten Indolizinen6‐8. Das mit einem aktivierten Seitenkettendipolarophil versehene Dicyanmethylid9liefert neben dem Indolizin11in geringen Mengen das Nap

ISSN:0365-6233    

DOI:10.1002/ardp.19933260803

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractSomeN,N′‐diacyl‐p‐phenylenediamines substituted with halogens (2a‐c) were prepared. Their polarographic reduction inN,N‐dimethylformamide with Et4NClO4was performed and discussed. The mechanism of the electrochemical reduction is stated. Large‐scale electrolytic reductions of2a‐bto3a

ISSN:0365-6233    

DOI:10.1002/ardp.19933260804

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThe synthesis of a series ofN‐(2‐chloroethyl)‐N′‐(9H‐xanthen‐9‐yl)‐N‐nitrosoureas andN‐(2‐chloroethyl)‐N′‐(9H‐thioxanthen‐9‐yl)‐N‐nitrosoureas is described. The title compounds were evaluated against NSCLCN6 L16 bronchial epidermoid carcinomain vitroand some of them were found to be active.N‐(2‐chloroethyl)‐N′‐(2‐methoxy‐9H‐xanthen‐9‐yl)‐N‐nitroso

ISSN:0365-6233    

DOI:10.1002/ardp.19933260805

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractAus den oberirdischen Teilen der Eberraute (Artemisia abrotanumL., Asteraceae) wurden neben (+)‐Davanon (1) und Arteinculton (3) die bekannten Peroxyhalbketale2,5und7isoliert. Als neue Peroxide vom Davanon‐Typ konnten Epi‐Arteinculton (4) und Spiro‐Arteinculton (6) durch dc Vergleich in der Pflanze nachgewiesen werden. Bei der Singulett‐Sauerstoff‐Oxidation von1werden2, 3, 4, 5und7gebildet, bei der Triplett‐Sauerstoff‐Oxidation2, 3, 5, 6, 7und

ISSN:0365-6233    

DOI:10.1002/ardp.19933260806

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThe new fMLP analog HCO‐Hmb‐Leu‐Phe‐OMe (1), containing (S)‐2‐hydroxy‐4‐(methylthio)butyric acid (Hmb) in place ofL‐methionine at theN‐terminal position, has been synthesized and fully characterized. The peptide1has been designed in order to improve the understanding of the role exerted by the formamido group in the binding interaction with the formylpeptide chemotactic receptors. Chemotaxis, superoxide anion production, and lysozyme release have been measured for both1and its deformylated analog Hmb‐Leu‐Phe‐OMe2. Results indicate that a strong hydrogen bond of the OH·…OC type may complement a weak H‐bonding interaction involving the

ISSN:0365-6233    

DOI:10.1002/ardp.19933260807

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

Abstract3‐Methoxy‐N,N′‐diaminophthalamide was observed to be a potent hypolipidemic agent in rodents. Serum cholesterol and triglyceride levels in rats were significantly reduced as were lipid contents of the liver, small intestine, and aorta wall. VLDL and LDL cholesterol levels were significantly reduced. Unfortunately, HDL cholesterol levels were also markedly reduced. Furthermore, acute toxicity studies showed that the compound caused marked increases in serum CP kinase activity with doses of 40 and 100 mg/kg/day in mice. This is not a property of the 2,3‐dihydrophthalazine‐1,4‐dione, the resultant product of theN,N′‐diaminophthalamides. Apparently, closing the ring results in a safer compound with elevations in HDL cholesterol levels, a desirable characteristic in effective hyp

ISSN:0365-6233    

DOI:10.1002/ardp.19933260808

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractDurch Kondensation vonN‐(2‐Hydroxyethyl)‐N‐methylguanidinsulfat (1) mit den 1‐Aryl‐substituierten β‐Diketonen4a‐eerhält man die bioisosteren 2‐[(2‐Hydroxyethyl)‐methylamino]‐6‐arylpyrimidine5a‐e. Die Verbindungen5a‐cbesitzen signifikante antimykotischei

ISSN:0365-6233    

DOI:10.1002/ardp.19933260809

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractPhenytoin‐1‐triglycerides and phenytoin‐2‐triglycerides were synthesized as potential prodrugs of phenytoin by covalent binding of 3‐hydroxymethylphenytoin by succinic acid to the positions 1 and 2 of diglycerides, respectively. The corresponding 1‐ and 2‐monoglycerides were prepared. In addition, replacement of glycerol by 3‐hydroxy‐2‐hydroxymethylpropionic acid furnished lipids that allowed direct coupling of 3‐hydroxyme‐thylphenytoin. The lipid conjugates proved to be substrates for pa

ISSN:0365-6233    

DOI:10.1002/ardp.19933260810

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractNine nitrosimino title compounds were prepared. They inhibit the aggregation of human platelets induced by collagen with an IC50= 0.7 ‐ 33 μmol/L. The most active substance is the 3‐phenylethyl derivative6b. Thein vitroeffect is mediated by an active metabolite which is formed by a photochemical reaction in the aggregometer. As the corresponding and so far unknown sydnone‐5‐cyanimines have no effect on platelets the metabolite is most certainly a NO‐species. The activity of the sydnone‐5‐nitrimine5bis in the same order of magnitude (IC50= 7.5 μmol/L) as in the nitrosimines of type6. The most active compound6bwas investigated for antithrombotic properties in a thrombosis model, where the thrombus formation was induced by a laserbeam. 2 h after oral administration of 60 mg/kg of6bto rats in venoles a 28% inhibition of thrombin formation was found. In arterioles this effect is more evident and a 48% inhibition is seen (the thrombus formation index is 2.6 and 3.9, respectively). These results suggest that the active metabolite is formed

ISSN:0365-6233    

DOI:10.1002/ardp.19933260811

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY