摘要:

AbstractCondensation of β‐aminocinnamic acid esters with 3‐chloro‐2‐methoxy‐crotonaldehyde opened an easy access to 2‐phenyl‐5‐methoxy‐4‐methylnicotinic acid esters which were cyclized by polyphosphoric acid to yield the corresponding 2‐methoxyonychines. By this method a number of 2‐methoxy‐substituted onychines were prepared for the first time, i.a. oxylopidine, the structure

ISSN:0365-6233    

DOI:10.1002/ardp.19943271202

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

Abstract2,6‐Dichloro‐4‐hydroxybenzylamine (1) and itsN‐methyl (2) andN‐ethyl (3) derivatives were synthesized and tested for estrogen receptor affinity as well as for estrogenic activity. In contrast to their related highly active 1,2‐bis(2,6‐dichloro‐4‐hydroxyphenyl)ethylenediamines (meso‐4‐meso‐6) none of the benzylamines showed hormonal activity. The coordination of the benzylamine1to platinum did not lead to an estrogenic compound. The reasons for the different activity of [meso‐1,2(bis‐2,6‐dichloro‐4‐hydroxyphenyl)ethylenediamine]dichloroplatium(II) (meso‐4‐PtCl2) andcis[bis(2,6‐dichloro‐4‐hydroxybenzylamine)]dichloroplatinum(II) (cis‐1‐PtCl2), the latter of which can be considered as a ring‐opened counterpart of the highly activemeso‐4‐PtCl2, are thoroughly discussed under inclusion of conformational facts. The results of this and the preceding work show, that the pharmacophoremeso‐1,2‐bis(2,6‐dichloro‐4‐hydroxyphenyl)ethylenediamine (meso‐4) which is exclusively responsible for the estrogenic activity ofmeso‐4‐PtCl2causes comparable hormonal effects in two different conformations with O‐O distances of about 8 Å (complex) and of about 12 Å (diamine)

ISSN:0365-6233    

DOI:10.1002/ardp.19943271203

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractThirty title compounds were prepared and tested for their antiplatelet activity in theBorn‐test. Five nitrosimines inhibit the aggregation induced by collagen in concentrations below 10 μmol/L halfmaximally. Four compounds were investigated in anin vivothrombosis model. An inhibition of thrombosis between 29 and 53% was observed in mesenteric arterioles of rats 2 h afterp.o.administration (60 mg/kg). The effect in venoles was less pronounced (10–22%). For one compound these effects could still be demonstrated 4 h after oral applica

ISSN:0365-6233    

DOI:10.1002/ardp.19943271204

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractA series of 4‐phenyl‐2‐thioxo‐benzo[4,5]thieno[2,3‐d]pyrimidine derivatives endowed with anti‐inflammatory and related pharmacological properties were submitted to a more extensive study to know their exact pharmacological profile and their possible side effects. The studied compounds possess a remarkable analgesic activity, devoid of central effects. They also show an interesting anti‐inflammatory profile evidenced by their effectiveness in different experimental models of inflammation. In addition, these compounds exhibit none or very little activity on CNS, scarce toxicity and low gastrointestina

ISSN:0365-6233    

DOI:10.1002/ardp.19943271205

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractThe absol. configuration of a Ciramadol analogue obtained from (‐)‐menthone is established by1H‐NMR‐, simulated NMR‐, COSY‐90‐, and NOE‐measurements. The final compound 2‐(α‐1‐pyrrolidino)benzyl‐4‐isopropyl‐1‐methyl‐cyclohexan‐3‐one (4b),e.g., has 1R,2S,4S,11S‐configuration due to stereoselectiveMichael‐type addition of pyrrolidine to

ISSN:0365-6233    

DOI:10.1002/ardp.19943271206

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractDie Nitroxid‐Radikale1eignen sich zumin situ‐Nachweis von Stickstoffmonoxid (NO˙), das unter aeroben Bedingungen aus dem Molsidomin‐Metaboliten SIN‐1 (3‐Morpholinosydnonimin) freigesetzt wird. Außer den stabilen Produkten2, 3und4entstehen bei dieser Reaktion auch die instabilen Aminoxyle5, die sich zu den stabilen Folgeprodukten3, 6und7zersetzen.7aentsteht auch bei der Reaktion vonlamitFentons‐Reagenz.7bläßt sich unabhängig durch Hexacyanoferrat(III)‐Oxidation aus dem Nitroxid8herstellen. Die Bildungsweise der Verbindungen2–5wird vor dem Hintergrund der relativen Reaktivität von1gegenüber Stickstoffmonoxid (NO˙) bzw. Stickstoffd

ISSN:0365-6233    

DOI:10.1002/ardp.19943271207

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractNω‐Hydroxy‐L‐arginine (2) was prepared by a multi‐stage synthesis; the key step was the addition of hydroxylamine to the protected cyanamide8. The presence ofN‐hydroxyguanidines was confirmed, above all, by15N‐NMR investigations.15Nω‐Hydroxy‐L‐arginine (2) was converted quantitatively to15NO by NO synthases from macrophages.15NO was identified by ESR‐spectroscopy. These experiments confirm that15Nω‐hydroxy‐L‐arginine (2) is an intermediate in the biosynthesis of NO from arginine (1) and that theN‐hydroxylated N‐

ISSN:0365-6233    

DOI:10.1002/ardp.19943271208

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

Abstract(R/S)‐Isochroman‐1‐carbonsäure (1) wird in ihre Enantiomere gespalten und ebenso wie diese mit 6‐Aminopenicillansäure zu den Titelverbindungen2umgesetzt. Die Wirkung der neuen Penicilline gegenüber grampositiven und gramnegativen Bakterien wird mit der von Benzylpenicillin

ISSN:0365-6233    

DOI:10.1002/ardp.19943271209

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractThe chemical synthesis of some related substances of the cephalosporin antibiotic cefadroxil is described. These compounds which may be present in commercial samples originate from the semisynthetic preparation of the antibiotic or from degradation. The preparation of these products enables the validation of selective quantitative analytical methods, such as liquid chromatography and tlc.

ISSN:0365-6233    

DOI:10.1002/ardp.19943271210

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY

摘要:

AbstractMifepristone (1) was found to be stable against ultraviolet light under the usual storage conditions. Upon irradiation for two weeks it gave two photoproducts, characterized as (11β, 17β)‐17‐Hydroxy‐11‐[4‐(methylamino)‐phenyl]‐17‐(1‐propinyl)‐19‐norandrosta‐4,9‐dien‐3‐one (2) and [5R,7E, 8R,8aR]‐5‐[4‐(dimethylamino)phenyl]‐4,5,6,7,8,8a,9,10‐octahydro‐7‐methyl‐8‐(3‐oxo‐4‐hexinyl)‐2(3H)‐phenanthrenone (3). Based on the crystal structure of1by X‐ray diffraction, the formation of2a

ISSN:0365-6233    

DOI:10.1002/ardp.19943271211

出版商:WILEY‐VCH Verlag    

年代:1994

数据来源: WILEY