ISSN:0365-6233    

DOI:10.1002/ardp.19933261202

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractOrale Antidiabetica vom Sulfonylsemicarbazid‐Typ wie Tolazamid (1) und Glisoxepid (2) wurden unter milden nitrosierenden Bedingungen, auch annähernd physiologischenin vitroBedingungen, nach einem neuartigen Reaktionsverlauf in Sulfonyltriazene3a, bumgewandelt. Modellverbindungen mitN4‐Acyl‐semicarbazidstruktur4zeigen abweichendes Reaktionsverhalten, wobei Säureamide5neben Nitrosaminen6gebildet

ISSN:0365-6233    

DOI:10.1002/ardp.19933261203

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

Abstract38 title compounds have been synthesized. They bear a wide variety in substituents including alkyl‐, aryl‐, arylalkyl‐, and styryl groups. The antiplatelet activities elucidated in theBorn‐test with collagen cover more than two orders of magnitude (IC50= 0.3‐45 μmol/L). These effects depend on the presence of theN‐NO‐group. This is shown by comparison with the corresponding sydnone imines, sydnone cyanimines, and sydnones. The most suitable substituents were phenylethyl, styryl, and hexyl at either position of the molecule. Seven compounds, most of them styryl derivatives, have IC50values below 1 μmol/L. It is suggested that the differences in activity are connected with the ability of the compounds to bind to the pl

ISSN:0365-6233    

DOI:10.1002/ardp.19933261204

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractDie α‐Methylen‐γ‐butyrolactone1‐28wurden auf molluskizide Wirkung gegenBiomphalaria glabratauntersucht. Die racem. Verbindung25ist am wirksamsten. Die Synthese erfolgte durch modifizierteReformatzky‐Reaktion aus den entspr. Carbonylverbindungen und Brommethylacrylsäureethylester.7‐10, 17und22‐27wurden erstmal

ISSN:0365-6233    

DOI:10.1002/ardp.19933261205

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

Abstract10ist ein β‐Carbolin‐Analogon des Neuroleptikums Flutrolin2a,b) mit deutlich geringerer Affinität zum Dopamin D2‐Rezeptor. Verschiedene Synthesewege zu10und die Molekülstruktur im Kristall von8werden beschrieben, Struktur‐Wirkungsbeziehungen, insbesondere die Bedeutung der “S‐shape” ‐ und rigidisierten Dopamin‐Kon

ISSN:0365-6233    

DOI:10.1002/ardp.19933261206

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractThe first phosphonoretinoic acid diethyl ester2was prepared byWittigreaction of the phosphonoaldehyde4and the ylide6. The aldehyde4was synthesized by smooth hydrolysis of the phosphonoacetal3with trifluoroacetic acid. The reaction of3with trimethylsilylbromide, hydrolysis, and precipitation resulted in salt5.

ISSN:0365-6233    

DOI:10.1002/ardp.19933261207

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractBy using the side chain to side chain mode of cyclization the 14‐membered disulfide cyclopeptide (5) has been synthesized as conformationally constrained analog of the prototypical chemotactic tripeptide For‐Met‐Leu‐Phe‐OMe. Compound5is inactive towards human neutrophils. The lack of biological activity of cyclotetrapeptide5is discussed taking into account the backbone folding and the side chain t

ISSN:0365-6233    

DOI:10.1002/ardp.19933261208

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractDie Mercaptopyridincarbonitrile1a‐dbzw. das Mercaptoisochinolincarbonitril1ereagieren mit 1,3‐Dichloraceton zu den Bisthioethern2a‐e. Durch basenkatalysierte Cyclisierung von2a‐ewerden die heterocyclisch substituierten Ketone3a‐eerhalten. Erhitzen von3abzw.3bin konz. H3PO4gibt die Bispyridothienopyridin

ISSN:0365-6233    

DOI:10.1002/ardp.19933261209

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractDifferent 1‐aryl‐2‐benzylmercapto‐4‐phenyl‐1,6‐dihydro‐1,3,5‐triazine‐6‐thiones have been synthesized by known methods. These triazines on treatment with ammonia/hydrazine hydrate afforded the corresponding 1‐aryl‐2‐amino/hydrazino‐4‐phenyl‐1,6‐dihydro‐1,3,5‐triazine‐6‐thiones which on treatment with arylisothiocyanates afforded the related thiocarbamides/thiosemicarbazides. Some of these compou

ISSN:0365-6233    

DOI:10.1002/ardp.19933261210

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY

摘要:

AbstractComplete three‐dimensional X‐ray crystal structure analyses of estrogenic [erythro‐1‐(2,6‐dichloro‐4‐hydroxyphenyl)‐2‐(2‐halo‐4‐hydroxyphenyl)ethylenediamine]diiodoplatinum(II) complexes (halo = fluoro:erythro8‐Ptl2and halo = chloro:erythro‐9‐PtI2) which were synthesized for application in breast and prostate cancer, have been carried out. 6239 as well as 6521 reflexes were measured and refined to an R‐value of 0.105 and 0.066, respectively. The molecules oferythro‐8‐PtI2are displaced laterally from a possible Pt‐Pt‐axis separated, alternatingly, by Pt‐Pt‐distances of 3.62 Å and 6.27 Å. A comparable structure possesseserythro‐9‐PtI2with Pt‐Pt‐distances of 3.59 Å and 6.32 Å.The ethylenediamine ligands oferythro‐8‐PtI2anderythro‐9‐PtI2are puckered and exist in half chair conformations. For both complexes the 2,6‐dichloro‐4‐hydroxyphenyl ring is equatorially arranged, while the 2‐halo‐4‐hydroxyphenyl ring is nearly perpendicular to the N‐Pt‐N plane. The O‐O‐distance between the phenolic oxygens amounts to 8.1 Å inerythro‐8‐PtI2and to 7.8 Å inerythro‐9‐PtI2. Though these O‐O‐distances differ strongly from that (12.1 Å), which is considered to be necessary for the binding of an estrogen to its receptor, [1‐(2,6‐dichloro‐4‐hydroxyphenyl)‐2‐(2‐halo‐4‐hydroxyphenyl)ethylenediamine)]platinum(II) complexes show estrogenic effects which are, however, strongly reduced compared to that of therapeutically used estrogens like diethylstilbestrol. The relationship between molecular structure and estrogenicity

ISSN:0365-6233    

DOI:10.1002/ardp.19933261211

出版商:WILEY‐VCH Verlag    

年代:1993

数据来源: WILEY