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Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry最新文献

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Synthesis of the potent mutagen 3,5,8-trimethyl-3H-imidazo[4,5-f]quinoxalin-2-amine. 强诱变剂3,5,8-三甲基- 3h -咪唑[4,5-f]喹诺沙林-2胺的合成
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-08-01 DOI: 10.3891/acta.chem.scand.40b-0583
T Nyhammar, S Grivas
{"title":"Synthesis of the potent mutagen 3,5,8-trimethyl-3H-imidazo[4,5-f]quinoxalin-2-amine.","authors":"T Nyhammar,&nbsp;S Grivas","doi":"10.3891/acta.chem.scand.40b-0583","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0583","url":null,"abstract":"<p><p>The mutagenic title compound (5,8-DiMeIQx) was synthesized by two different routes: from 2-methyl-4,6-dinitroaniline; and from 4-chloro-2-methyl-6-nitroaniline. The latter and more convenient route involved 2,1,3-benzoselenadiazole intermediates.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 7","pages":"583-7"},"PeriodicalIF":0.0,"publicationDate":"1986-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14883898","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: 9
Misincorporation of alkylated amino acids into hemoglobin--a possible source of background alkylations. 错误地将烷基化氨基酸掺入血红蛋白——可能是烷基化背景的来源。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-07-01 DOI: 10.3891/acta.chem.scand.40b-0453
A Kautiainen, S Osterman-Golkar, L Ehrenberg
{"title":"Misincorporation of alkylated amino acids into hemoglobin--a possible source of background alkylations.","authors":"A Kautiainen,&nbsp;S Osterman-Golkar,&nbsp;L Ehrenberg","doi":"10.3891/acta.chem.scand.40b-0453","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0453","url":null,"abstract":"<p><p>Misincorporation of 2-hydroxyethylated amino acids into hemoglobin during de novo synthesis was studied by injecting mice with radiolabelled N-(2-hydroxyethyl)valine, S-(2-hydroxyethyl)cystine or N tau-(2-hydroxyethyl)histidine. The results showed that S-(2-hydroxyethyl)cysteine and N tau-(2-hydroxyethyl)histidine were misincorporated, whereas N-(2-hydroxyethyl)valine was not. Monitoring of in vivo doses of hydroxyethylating agents by determination of N-(2-hydroxyethyl)valine was free of the disturbing influence of such misincorporation.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 6","pages":"453-6"},"PeriodicalIF":0.0,"publicationDate":"1986-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14884850","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: 21
Evidence against in vitro modulation of rat liver cholesterol 7 alpha-hydroxylase activity by phosphorylation-dephosphorylation: comparison with hydroxymethylglutaryl CoA reductase. 磷酸化-去磷酸化对大鼠肝脏胆固醇7 α -羟化酶活性的体外调节的证据:与羟甲基戊二酰辅酶a还原酶的比较。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-07-01 DOI: 10.3891/acta.chem.scand.40b-0457
L Berglund, I Björkhem, B Angelin, K Einarsson
{"title":"Evidence against in vitro modulation of rat liver cholesterol 7 alpha-hydroxylase activity by phosphorylation-dephosphorylation: comparison with hydroxymethylglutaryl CoA reductase.","authors":"L Berglund,&nbsp;I Björkhem,&nbsp;B Angelin,&nbsp;K Einarsson","doi":"10.3891/acta.chem.scand.40b-0457","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0457","url":null,"abstract":"<p><p>The activity of cholesterol 7 alpha-hydroxylase in rat liver microsomes was investigated under conditions favourable for phosphorylation-dephosphorylation. The enzyme activity was similar in the presence or absence of sodium fluoride during preparation. Preincubation with ATP and magnesium did not affect the enzyme activity. Cholesterol 7 alpha-hydroxylase was inhibited by alkaline phosphatase, but this inhibition was similar also after inactivation of the phosphatase. Under similar conditions, rat hepatic hydroxymethylglutaryl CoA reductase activity was clearly modulated in agreement with phosphorylation-dephosphorylation. The absence of such a modulation of cholesterol 7 alpha-hydroxylase argues against involvement of phosphorylation-dephosphorylation in the regulation of this enzyme.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 6","pages":"457-61"},"PeriodicalIF":0.0,"publicationDate":"1986-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14884851","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
Efficient synthesis of mutagenic imidazo[4,5-f] quinoxalin-2-amines via readily accessible 2,1,3-benzoselenadiazoles. 通过易于获取的2,1,3-苯并硒二唑高效合成致突变性咪唑[4,5-f]喹诺沙林-2胺。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-05-01
S Grivas
{"title":"Efficient synthesis of mutagenic imidazo[4,5-f] quinoxalin-2-amines via readily accessible 2,1,3-benzoselenadiazoles.","authors":"S Grivas","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 5","pages":"404-6"},"PeriodicalIF":0.0,"publicationDate":"1986-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14869400","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
On the mechanism of the pseudocatalatic degradation of hydrogen peroxide by lactoperoxidase/iodide. 乳过氧化物酶/碘化物假催化降解过氧化氢的机理研究。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-05-01 DOI: 10.3891/acta.chem.scand.40b-0358
P I Ohlsson
{"title":"On the mechanism of the pseudocatalatic degradation of hydrogen peroxide by lactoperoxidase/iodide.","authors":"P I Ohlsson","doi":"10.3891/acta.chem.scand.40b-0358","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0358","url":null,"abstract":"<p><p>Hydrogen peroxide is catalytically disproportionated by lactoperoxidase in the presence of iodide ions, Km = 55 microM in 100 mM sodium phosphate, pH 7.00, 25 degrees C. Products formed are water and molecular oxygen. The reaction is competitively inhibited by hydrogen sulfite, Ki = 0.24 mM in 100 mM sodium phosphate, pH 7.00, 25 degrees C. The stoichiometry of the reaction is identical with the corresponding catalase reaction but the mechanism differs. A mechanistic model for lactoperoxidase-iodide dismutation of hydrogen peroxide is discussed.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 5","pages":"358-62"},"PeriodicalIF":0.0,"publicationDate":"1986-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14869399","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
N-methyl-N'-nitro-N-nitrosoguanidine and cyclic GMP stimulate phosphorylation of nuclear proteins from rat liver. n -甲基-n '-硝基-n -亚硝基胍和环GMP刺激大鼠肝脏核蛋白磷酸化。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-05-01 DOI: 10.3891/acta.chem.scand.40b-0390
E Danielsson, O Nordström, T Bartfai
{"title":"N-methyl-N'-nitro-N-nitrosoguanidine and cyclic GMP stimulate phosphorylation of nuclear proteins from rat liver.","authors":"E Danielsson,&nbsp;O Nordström,&nbsp;T Bartfai","doi":"10.3891/acta.chem.scand.40b-0390","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0390","url":null,"abstract":"","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 5","pages":"390-3"},"PeriodicalIF":0.0,"publicationDate":"1986-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14012812","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
Efficient synthesis of mutagenic imidazo[4,5-f] quinoxalin-2-amines via readily accessible 2,1,3-benzoselenadiazoles. 通过易于获取的2,1,3-苯并硒二唑高效合成致突变性咪唑[4,5-f]喹诺沙林-2胺。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-05-01 DOI: 10.3891/ACTA.CHEM.SCAND.40B-0404
S. Grivas
{"title":"Efficient synthesis of mutagenic imidazo[4,5-f] quinoxalin-2-amines via readily accessible 2,1,3-benzoselenadiazoles.","authors":"S. Grivas","doi":"10.3891/ACTA.CHEM.SCAND.40B-0404","DOIUrl":"https://doi.org/10.3891/ACTA.CHEM.SCAND.40B-0404","url":null,"abstract":"","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"172 1","pages":"404-6"},"PeriodicalIF":0.0,"publicationDate":"1986-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76677439","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: 12
Synthesis of a putative antigenic heptapeptide from Escherichia coli K88 ab protein fimbriae. 从大肠杆菌k88ab蛋白菌毛中合成推定的抗原七肽。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-04-01 DOI: 10.3891/acta.chem.scand.40b-0250
M Meldal
{"title":"Synthesis of a putative antigenic heptapeptide from Escherichia coli K88 ab protein fimbriae.","authors":"M Meldal","doi":"10.3891/acta.chem.scand.40b-0250","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0250","url":null,"abstract":"<p><p>The heptapeptide Tyr-Arg-Glu-Asp-Met-Glu-Tyr-OMe, spanning region 213-219 of Escherichia coli K88 ab protein fimbriae, was synthesized with an overall yield of 37% using dicyclohexylcarbodiimide (DCC) and 1-hydroxybenzotriazole (HOBt) preactivation in all condensation reactions. The C-terminal was protected as the methyl ester. The protection scheme of N alpha-tert-butyloxycarbonyl-(Boc) and benzyl-(Bzl) or benzyloxycarbonyl (Z) groups for side chain protection was found to be orthogonal when a mixture of trifluoroacetic acid (TFA), phenol (PhOH) and p-cresol (CrOH) was used for repetitive deprotection. The final deprotection of Boc-Tyr(Bzl)-Arg(Z2)-Glu(Bzl)-Asp(Bzl)-Met-Glu(Bzl+ ++)-Tyr(Bzl)-OMe (17) was accomplished in 80% yield by prolonged treatment with hydrogen fluoride, dimethyl sulfide, p-cresol and p-thiocresol. The BSA-linked synthetic peptide was used in immunisation experiments on rabbits.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 4","pages":"250-6"},"PeriodicalIF":0.0,"publicationDate":"1986-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14008860","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
Design and synthesis of antagonists of substance P. P物质拮抗剂的设计与合成。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-04-01 DOI: 10.3891/acta.chem.scand.40b-0295
K Folkers, S Rosell, J Y Chu, L A Lu, P F Tang, A Ljungqvist
{"title":"Design and synthesis of antagonists of substance P.","authors":"K Folkers,&nbsp;S Rosell,&nbsp;J Y Chu,&nbsp;L A Lu,&nbsp;P F Tang,&nbsp;A Ljungqvist","doi":"10.3891/acta.chem.scand.40b-0295","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0295","url":null,"abstract":"<p><p>Synthesis and bioassay of about 65 analogs of substance P (SP) over five years yielded the antagonist [D-Arg1,D-Trp7,9,Leu11]-SP, which was named Spantide, and which was used by many investigators as a \"tool\". Spantide served as a reference antagonist for the design of 47 new peptides toward the goal of more potent inhibitors. Designs emphasized analogs with D-Trp7, D-Trp9, D-Trp10, D-pClPhe10, Nle11, Leu11, Ile11 and Met11, etc. Twenty-one/47 antagonists were superior in potency to that of Spantide, the best was [D-Arg1,D-Na1(5), D-Trp7,9,Nle11]-SP which required a 255-fold increase in SP concentration to give 50% of the maximum response at a concentration of 10(-5)M of the antagonist; this potency is ca. 5 times that of Spantide. For certain, but not all pairs of undecapeptides and truncated analogs, the undecapeptides may be significantly more potent than the truncated counterparts.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 4","pages":"295-302"},"PeriodicalIF":0.0,"publicationDate":"1986-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13571937","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: 13
Synthesis of a putative subtype specific antigenic heptapeptide from Escherichia coli K88 ad protein fimbriae. 从大肠杆菌K88蛋白菌毛中合成一种假定的亚型特异性抗原七肽。
Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry Pub Date : 1986-04-01 DOI: 10.3891/acta.chem.scand.40b-0242
M Meldal
{"title":"Synthesis of a putative subtype specific antigenic heptapeptide from Escherichia coli K88 ad protein fimbriae.","authors":"M Meldal","doi":"10.3891/acta.chem.scand.40b-0242","DOIUrl":"https://doi.org/10.3891/acta.chem.scand.40b-0242","url":null,"abstract":"<p><p>The heptapeptide methyl ester Phe-Asn-Glu-Asn-Met-Ala-Tyr-OMe covering the amino acid sequence of the region 213-219 of Escherichia Coli K88 ad protein fimbriae is synthesized using N alpha-t-butyloxycarbonyl-protection and benzyl groups for side-chain-protection. All condensation reactions are performed in 84-97% yield by preactivation of the protected amino acids by dicyclohexylcarbodiimide (DCC) and 1-hydroxybenzotriazole (HOBt), and reaction of the resulting active ester with amine in the presence of 4-methylmorpholine (NMM). A mechanism is proposed for the nitrile formation in the side-chain of activated asparagine, and the suppression of this side-reaction is investigated. The repetitive deprotection is performed in a mixture of trifluoroacetic acid (TFA), phenol and p-cresol to give the TFA salts in virtually quantitatively yields. The final deprotection of the heptapeptide is carried out in a mixture of 25% hydrogen fluoride (HF) and dimethyl sulfide (DMS) in an overall yield of 48%. The serological and conformational properties of the synthetic peptide are under investigation.</p>","PeriodicalId":6886,"journal":{"name":"Acta chemica Scandinavica. Series B: Organic chemistry and biochemistry","volume":"40 4","pages":"242-9"},"PeriodicalIF":0.0,"publicationDate":"1986-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14008859","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: 9
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