摘要:

AbstractEs wird über die Synthese der Alkyliden‐α‐thiotetronsäuren11und12aund mehrere ihrer Derivate berichtet. Ausgangsverbindungen sind das 2,3‐Dimethoxybernsteinsäure‐thioanhydrid (4) sowie Thioacetondicarbonsäureester. Bei der Rhodium(II)‐katalysierten Zersetzung des Diazoketons26entsteht das Redukton12pund das Aminoredukton12r. Eines der Nebenprodukte ist d

ISSN:0365-6233    

DOI:10.1002/ardp.19953280202

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractAccording to a recent hypothesis suggesting the potential role of free radical formation in the clozapine‐induced agranulocytosis, we have evaluated the susceptibility to the peroxidase‐mediated oxidation of different dibenzazepine analogues. On the one hand, compounds with an arylamine group such as clozapine present a high reactivity in the horseradish peroxidase or myeloperoxidase systems and, on the other hand, fluperlapine, though known to induce agranulocytosis, and other debenzothiazepine and dibenzoxazepine derivatives appear insensitive to oxidation. Consequently, among tricyclic derivatives, the way of diaryloxa‐ and diarylthiazepine compounds could be an alternative for the development of safer drugs such as antipsych

ISSN:0365-6233    

DOI:10.1002/ardp.19953280203

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe preparation of immunologically active phthalimido desmuramylpeptide analogues2e‐h, 4c‐d, and7bis described. TheN‐acetylmuramic acid in the muramyl dipeptide has been replaced by a phthaloylated acyclic moiety such asN‐phthaloylated amino acids1a–c, 2‐(2‐phthalimidoethoxy)acetic acid3, or by the carbocyclic rac.trans‐2‐(2′‐phthalimidocyclo

ISSN:0365-6233    

DOI:10.1002/ardp.19953280204

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractCyclization ofN‐[5‐(4‐chlorobenzylidene]‐4‐oxo‐2‐imidazolidinyl]glycine (4) in acetic acid anhydride yielded 1‐acetyl‐6‐(4‐chlorobenzylidene)‐2,3,5,6‐tetrahydroimidazo[2,1‐b]imidazole‐3,5‐dione (5). The structure of5was ascribed on basis of its MS,1H‐ and13C‐NMR properties. The crystal structure of5was solved by X‐ray analysis. On the basis of semiempirical quantum chemistry calculations (PM3 method) the thermodynamic stability of theoretically possible cyclization products was determined. These data allow to predict the direction of cyclization. The stability and the reactivity of5tow

ISSN:0365-6233    

DOI:10.1002/ardp.19953280205

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe oligoamine RE 1492C (N,N′,N″ ‐4‐phenylbutyl‐1,3,5‐benzene‐trimethanamine‐N,N′,N″ ‐triethylcarbamate) inhibited the electrically provoked leucocyte adhesion to the endothelium of rat mesenteric venoles. An oral dose of 60 mg/kg gave a significant inhibition of 65–78%. This is comparable to effects seen after i.v. administration of iloprost or PGE1, respectively. In the same dosage the NO‐donor RE 2047 (3‐methyl‐N‐nitroso‐sydnone‐5‐im

ISSN:0365-6233    

DOI:10.1002/ardp.19953280206

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractDimethindene and its metaboliteN‐demethyldimethindene were determined in human urine after dermal administration of dimethindene. The HPLC‐method used was previously described. Data of 8 volunteers are presented. After 32 h an average of 0.023% of the administered dose of dimethindene and 0.022% ofN‐demethyldimethindene were excreted into urine. Since also after oral administration of dimethindene only about 1% of unmetabolised dimethindene is found in urine it can be concluded that a certain amount of dimethindene is absorbed through the skin after dermal administr

ISSN:0365-6233    

DOI:10.1002/ardp.19953280207

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractFifteen fluorescent oligoamines with one or two fluorescent groups and two or three basic N‐functions were prepared and tested for antiplatelet activity (Born‐test). Five compounds involving three different fluorophores,i.e.2‐fluorenyl, 1‐pyrenyl, and 9‐phenanthryl, show an IC50of 7–11 μmol/L. They are suitable to serve as probes in the field of oligoamine‐biopolymer

ISSN:0365-6233    

DOI:10.1002/ardp.19953280208

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractMesoionic 1,2,3,4‐oxatriazolimines and the corresponding oxatriazolones were prepared and tested for their antiplatelet and antithrombotic activities. In theBorn‐test 5‐amino‐3‐phenyl‐1,2,3,4‐oxatriazolimine chloride inhibited the platelet aggregation halfmaximally in a concentration of 50 nmol/L. ItsN‐ethoxycarbonyl derivative inhibited thrombus formation in arterioles of rats by 48% (10 mg/kg, 2 h after p.o. administration). These effects appear to be related to the formation of intermediate nitrosohydrazine derivatives. This aspect was supported by the activities in noncyclic nitrosohydrazines (2 compds.), nitrosohydrazones (2) and nitrosohydrazides (11). Five of them exhibited an IC50<100 nmol/L in theBorn‐test. In a thrombotic model strong inhibition of thrombus formation was observed after intravenous application. The 1‐nitroso‐1‐benzylhydrazine even exhibited strong inhibitory effects af

ISSN:0365-6233    

DOI:10.1002/ardp.19953280209

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractThe 5‐HT1aand 5‐HT2receptor affinity of a set of 44N‐alkylated 1‐arylpiperazines and their analogs has been analyzed: then‐hexyl derivatives were the most potent and the most selective 5‐HT1aligands of all the investigatedN‐alkyl homologues. The alkyl chain may stablize the 5‐HT1areceptor‐ligand complex by hydrophobic forces. A set of the alkyl substituent contributions (Cht1a) for prediction of the 5‐HT1aaffinity ofN‐alkyl derivatives of 1‐arylpiperazines and related compounds have been defined on the basis of

ISSN:0365-6233    

DOI:10.1002/ardp.19953280210

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY

摘要:

AbstractAusgehend vomMannich‐Salz1des Aldosteronantagonisten Canrenon oder von 2‐Methylen‐canrenon (2) wurden die am A‐Ring anellierten Hetero‐ und Carbocyclen5, 6,8–13dargestellt. Mit den Verbindungen2, 3, 4b, 5, 6b, 8und12wurden Bindungsstudien am Estradiol‐, Progesteron‐, Androgen‐, Glucocorticoid‐ und Mineralocorticoid‐Rezeptor sowie an den Serumproteinen Sexualhormonbindendes Globulin (SHBG) und Corticosteroidbindendes Globulin (CBG) durchgeführt. Die relativen Bindungsaffinitäten lagen bei CBG unter 1%, in allen anderen Fä

ISSN:0365-6233    

DOI:10.1002/ardp.19953280211

出版商:WILEY‐VCH Verlag    

年代:1995

数据来源: WILEY