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Acta chemica Scandinavica (Copenhagen, Denmark : 1989)最新文献

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Synthesis of prodrugs as bridged nucleosides. 作为桥接核苷的前药的合成。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-10-01 DOI: 10.3891/acta.chem.scand.52-1270
J Hatlelid, T Benneche, K Undheim
{"title":"Synthesis of prodrugs as bridged nucleosides.","authors":"J Hatlelid,&nbsp;T Benneche,&nbsp;K Undheim","doi":"10.3891/acta.chem.scand.52-1270","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-1270","url":null,"abstract":"<p><p>Methods for the preparation of N,N'-connected bisnucleosides have been developed. The bridge is formally a carbonate ester of N-hydroxymethyl nucleosides. Both symmetrical and non-symmetrical bridged bisnucleosides are available.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 10","pages":"1270-4"},"PeriodicalIF":0.0,"publicationDate":"1998-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20696917","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Unification of some literature models of aromaticity: calculational and conceptual study of a set of one-ring species. 一些文献芳香性模型的统一:一组单环种的计算和概念研究。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-08-01 DOI: 10.3891/acta.chem.scand.52-0967
A Skancke, R S Hosmane, J F Liebman
{"title":"Unification of some literature models of aromaticity: calculational and conceptual study of a set of one-ring species.","authors":"A Skancke,&nbsp;R S Hosmane,&nbsp;J F Liebman","doi":"10.3891/acta.chem.scand.52-0967","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0967","url":null,"abstract":"<p><p>Numerous models have been suggested for the important concept of aromaticity. In the current study, a set of recently suggested models of aromaticity/homoaromaticity/anti-aromaticity for one-ring species [e.g. pyridazine, oxazole, tropilidene (cycloheptatriene), 1,4-dithiin, [8]-annulene (cyclooctatetraene)] is shown to have a common mathematical framework from which a new, unifying quantitative equation has been derived. Calculational and conceptual application is made to a well defined set of one-ring carbocycles.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 8","pages":"967-74"},"PeriodicalIF":0.0,"publicationDate":"1998-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20608831","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 14
Chaperone properties of calreticulin. 钙网蛋白的伴侣性。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-07-01
C Svaerke, G Houen
{"title":"Chaperone properties of calreticulin.","authors":"C Svaerke,&nbsp;G Houen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Calreticulin is a highly conserved protein with a relative molecular weight of 46,000, and is mainly located in the endoplasmic reticulum. Calreticulin was first characterized as a calcium-binding protein in the endoplasmic reticulum, but since then other functions of calreticulin have been characterized, including chaperone and lectin properties, and regulation of integrin and nuclear hormone receptor activity. We have investigated the interactions between purified human placental calreticulin and native and denatured proteins. Our results show that calreticulin binds to denatured proteins in a time- and pH-dependent manner, which at physiological pH is dependent on divalent cations. The binding was dependent on the state of the denatured protein, and was highly sensitive to the ionic composition of the environment, being strongly inhibited by phosphate-containing compounds. Calreticulin did not seem to distinguish between denatured glycosylated and non-glycosylated proteins, and was found to bind to native basic proteins, presumably by sheer electrostatic forces.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 7","pages":"942-9"},"PeriodicalIF":0.0,"publicationDate":"1998-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20580380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Polyamine-stimulated binding of diamine oxidase to DNA. 多胺刺激二胺氧化酶与DNA的结合。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-07-01 DOI: 10.3891/acta.chem.scand.52-0921
L Bruun, E V Hłgdall, J Vuust, G Houen
{"title":"Polyamine-stimulated binding of diamine oxidase to DNA.","authors":"L Bruun,&nbsp;E V Hłgdall,&nbsp;J Vuust,&nbsp;G Houen","doi":"10.3891/acta.chem.scand.52-0921","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0921","url":null,"abstract":"<p><p>Diamine oxidase is a Cu-containing enzyme which intracellularly participates in the regulation of the levels of putrescine, spermidine and spermine and in this process produces growth inhibitory amino aldehydes and hydrogen peroxide. Extracellularly, the enzyme participates in the inactivation of biogenic amines, notably histamine. Here we present evidence that in the presence of polyamines, diamine oxidase has the ability to bind DNA and to oxidise DNA-bound polyamines. The enzyme associates with chromosomal DNA since it can be released from human placental DNA by treatment with DNase I and it may be involved in the degradation of DNA. Thus, diamine oxidase may belong to a new class of DNA-binding proteins.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 7","pages":"921-9"},"PeriodicalIF":0.0,"publicationDate":"1998-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20580378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Synthesis of 3'-azolyl-2',3'-dideoxyhexose nucleosides. 3′-偶氮基-2′，3′-二脱氧己糖核苷的合成。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-07-01 DOI: 10.3891/acta.chem.scand.52-0935
K Walczak, E B Pedersen, C Nielsen
{"title":"Synthesis of 3'-azolyl-2',3'-dideoxyhexose nucleosides.","authors":"K Walczak,&nbsp;E B Pedersen,&nbsp;C Nielsen","doi":"10.3891/acta.chem.scand.52-0935","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0935","url":null,"abstract":"<p><p>1,8-Diazabicyclo[5.4.0]undec-7-ene salts of 2-methyl-4(5)-nitroimidazole or benzotriazole were obtained in crystalline form. Michael-type addition of these salts to (4S,5R)-(E)-4,6-di-O-acetyl-5-hydroxy-2-hexenal gave, after acetylation of the product, an isomeric mixture of acetylated 3-(azol-1-yl)-2,3-dideoxy-D-arabino-hexopyranosides and 3-(azol-1-yl)-2,3-dideoxy-D-ribo-hexofuranosides. Reaction of these peracetylated adducts with trimethylsilylated thymine in the presence of trimethylsilyl trifluoromethanesulfonate (TMS triflate) afforded the corresponding nucleosides which were deprotected by using methanolic ammonia. The nucleosides were found inactive against HIV-1 and HSV-1.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 7","pages":"935-41"},"PeriodicalIF":0.0,"publicationDate":"1998-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20580379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
Cladobotryal: a fungal metabolite with a novel ring system. 枝孢体:一种具有新型环系统的真菌代谢物。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-05-01 DOI: 10.3891/acta.chem.scand.52-0631
J Breinholt, H C Jensen, A Kjaer, C E Olsen, B R Rassing, C N Rosendahl, I Søtofte
{"title":"Cladobotryal: a fungal metabolite with a novel ring system.","authors":"J Breinholt,&nbsp;H C Jensen,&nbsp;A Kjaer,&nbsp;C E Olsen,&nbsp;B R Rassing,&nbsp;C N Rosendahl,&nbsp;I Søtofte","doi":"10.3891/acta.chem.scand.52-0631","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0631","url":null,"abstract":"<p><p>In screening for antifungal metabolites a novel compound, cladobotryal, was isolated from the mycoparasitic fungus Cladobotryum varium. Its structure was established as (+)-(2R*,3R*)-2-[(Z)-2-buten-2-yl]-3, 7-dihydro-3-formyl-3-methyl-5-phenylfuro[2,3-b]pyridin-4(2H)-one on the basis of spectroscopic evidence and single crystal X-ray analysis of its methyl hemiacetal. The fused furo[2,3-b]pyridinone skeleton of cladobotryal seems unprecedented within the chemical literature.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 5","pages":"631-4"},"PeriodicalIF":0.0,"publicationDate":"1998-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20507196","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 14
Synthesis of 11C/13C-labelled prostacyclins. 11C/ 13c标记的前列环素的合成。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-05-01 DOI: 10.3891/acta.chem.scand.52-0635
M Björkman, Y Andersson, H Doi, K Kato, M Suzuki, R Noyori, Y Watanabe, B Långström
{"title":"Synthesis of 11C/13C-labelled prostacyclins.","authors":"M Björkman,&nbsp;Y Andersson,&nbsp;H Doi,&nbsp;K Kato,&nbsp;M Suzuki,&nbsp;R Noyori,&nbsp;Y Watanabe,&nbsp;B Långström","doi":"10.3891/acta.chem.scand.52-0635","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0635","url":null,"abstract":"<p><p>A one-pot synthesis of (15R)-16-(3-[11C]methylphenyl)-17,18,19, 20-tetranoriso-carbacyclin methyl ester was performed using a palladium-promoted reaction of [11C]methyl iodide with (15R)-16-(3-tri-n-butylstannylphenyl)-17,18,19, 20-tetranorisocarbacyclin methyl ester. The C-15 epimer (15S)-16-(3-[11C]methylphenyl)-17,18,19,20-tetranorisocarbacyclin methyl ester was synthesised in the same way starting from (15S)-16-(3-tributylstannylphenyl)-17,18,19,20-tetranorisocarba cyclin methyl ester. The decay-corrected radiochemical yields were 33-45% based on [11C]methyl iodide produced, and the radiochemical purity of the product was > 95%. The total synthesis time was 35 min, counted from end of radionuclide production to product ready for administration. The 11C-labelled prostacyclin methyl esters were easily hydrolysed using sodium hydroxide affording the 11C-labelled prostacyclin acids in quantitative yields. The stereoisomers (15R)-16-(3-methylphenyl)-17,18,19,20-tetranorisocarbacyclin [11C]methyl ester and (15S)-16-(3-methylphenyl)-17,18,19,20-tetranorisocarbacyclin [11C]methyl ester were synthesised by esterification using [11C]methyl iodide and the tetrabutylammonium salts of (15R)-16-(3-methylphenyl)-17,18,19,20-tetranorisocarbacyclin acid and (15S)-16-(3-methylphenyl)-17,18,19,20-tetranorisocarbacyclin acid, respectively. The decay-corrected radiochemical yields were in the range of 55% counting from [11C]methyl iodide produced, and the radiochemical purity of the product was > 95%. The total synthesis time was 35 min, counting from end of radionuclide production to product ready for administration. Both of these labelling methods can be used for labelling with 13C when (13C)methyl iodide is used. The methods described herein have already proved important since they enable the in vivo use of PET to study the action of prostacyclins in the brain.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 5","pages":"635-40"},"PeriodicalIF":0.0,"publicationDate":"1998-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20507197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 32
Synthesis of meiosis-activating sterols containing fluorine. 含氟减数分裂激活甾醇的合成。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-04-01 DOI: 10.3891/acta.chem.scand.52-0503
M Wenckens, F Grønvald, J B Hansen
{"title":"Synthesis of meiosis-activating sterols containing fluorine.","authors":"M Wenckens,&nbsp;F Grønvald,&nbsp;J B Hansen","doi":"10.3891/acta.chem.scand.52-0503","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0503","url":null,"abstract":"<p><p>It is documented that specific types of sterol play a major role in the resumption of meiosis in oocytes from mice in vitro. 4,4-Dimethyl-5 alpha-cholesta-8,14,24-trien-3 beta-ol (FF-MAS) isolated from human follicular fluid and 4,4-dimethyl-5 alpha-cholesta-8,24-dien-3 beta-ol (T-MAS) isolated from bull testicular tissue, have been shown to activate (promote) meiosis in vitro. In order to evaluate the biological activity and stability of such compounds, new demethylsterol derivatives have been synthesised. Using diethylaminosulfur trifluoride (DAST) it was possible to synthesise selected delta 8, delta 14 sterols with mono and difluoro substitution at C3.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 4","pages":"503-7"},"PeriodicalIF":0.0,"publicationDate":"1998-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20472093","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
A study of baker's yeast reduction of piperidone-carboxylates. 面包酵母还原胡椒酮羧酸盐的研究。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-04-01 DOI: 10.3891/acta.chem.scand.52-0461
M Willert, M Bols
{"title":"A study of baker's yeast reduction of piperidone-carboxylates.","authors":"M Willert,&nbsp;M Bols","doi":"10.3891/acta.chem.scand.52-0461","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0461","url":null,"abstract":"<p><p>The stereoselective baker's yeast reduction of various N-protected piperidone-carboxylic acids have been studied, and the enantioselectivity was found to be widely dependent on whether fermenting or non-fermenting conditions were employed. Thus reaction of N-tert-butoxycarbonyl-4-oxopiperidine-3-carboxylic acid ethyl ester (6) with fermenting baker's yeast gave almost racemic N-tert-butoxycarbonyl-4-hydroxypiperidine-3-carboxylic acid ethyl ester (7), however, with complete diastereoselectivity. Reduction of 6 with non-fermenting yeast gave 7 with a 24-41% enantiomeric excess. Similarly, reduction of N-tert-butoxycarbonyl-3-oxopiperidine-4-carboxylic acid ethyl ester (17) with fermenting baker's yeast gave racemic N-tert-butoxycarbonyl-3-hydroxypiperidine-4-carboxylic acid ethyl ester [(+/-)-18] diastereoselectively. A convenient method for determining the enantiomeric excess of the hydroxypiperidine carboxylic acids derivatives was found in the reaction with Sanger's reagent followed by HPLC on a chiral column.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 4","pages":"461-8"},"PeriodicalIF":0.0,"publicationDate":"1998-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20471601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 10
Synthesis of substituted chiral piperazones resembling aza-sugars. 类似氮杂糖的取代手性哌酮的合成。
Acta chemica Scandinavica (Copenhagen, Denmark : 1989) Pub Date : 1998-04-01 DOI: 10.3891/acta.chem.scand.52-0499
A Lohse, B V Ernholt, M Bols
{"title":"Synthesis of substituted chiral piperazones resembling aza-sugars.","authors":"A Lohse,&nbsp;B V Ernholt,&nbsp;M Bols","doi":"10.3891/acta.chem.scand.52-0499","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.52-0499","url":null,"abstract":"<p><p>(6R)-6-(Hydroxymethyl)piperazin-2-one (1), (6S)-6-(hydroxymethyl)piperazin-2-one (2) and (6S)-6-[(1R, 2S, 3R)-1,2,3,4-tetrahydroxybutyl]piperazin-2-one (3) have been prepared in optically pure forms starting from D-glucosamine hydrochloride (4). The compounds (1-3) were tested for glycosidase inhibition.</p>","PeriodicalId":76966,"journal":{"name":"Acta chemica Scandinavica (Copenhagen, Denmark : 1989)","volume":"52 4","pages":"499-502"},"PeriodicalIF":0.0,"publicationDate":"1998-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"20472091","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
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