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Il Farmaco; edizione scientifica最新文献

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Biological study of triterpenequinones from celastraceae. 天竺葵科植物三萜醌的生物学研究。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
A G Gonzáles, A G Ravelo, I L Bazzocchi, J Jimenes, C M Gonzáles, J G Luis, E A Ferro
{"title":"Biological study of triterpenequinones from celastraceae.","authors":"A G Gonzáles,&nbsp;A G Ravelo,&nbsp;I L Bazzocchi,&nbsp;J Jimenes,&nbsp;C M Gonzáles,&nbsp;J G Luis,&nbsp;E A Ferro","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The cytostatic activity of several triterpenequinone methides isolated from Rzedowskia tolantonguensis and Maytenus horrida (Celastraceae) was evaluated against HeLa cell cultures. Their ID50 were determined and compared with those of other related compounds. A preliminary study of the antibacterial activity of the above triterpenequinone methides was also carried out.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"501-5"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14339666","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
Formation of 2,6-dimethoxy-1,4-benzoquinone, a highly genotoxic compound, from the reaction of sodium nitrite with the sympathomimetic drug dimethophrine in acidic aqueous solution. 亚硝酸钠与拟交感神经药物二甲氧嘧啶在酸性水溶液中反应生成高度遗传毒性化合物2,6-二甲氧基-1,4-苯醌。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
M Mazzei, G Roma, A Balbi, E Sottofattori, L Robbiano
{"title":"Formation of 2,6-dimethoxy-1,4-benzoquinone, a highly genotoxic compound, from the reaction of sodium nitrite with the sympathomimetic drug dimethophrine in acidic aqueous solution.","authors":"M Mazzei,&nbsp;G Roma,&nbsp;A Balbi,&nbsp;E Sottofattori,&nbsp;L Robbiano","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Because of the genotoxic effects shown by Dimethophrine (DMP) nitrosation mixtures, the interaction between DMP hydrochloride and sodium nitrite in acidic aqueous solution at 37 degrees was investigated in a wide range of reagent concentrations and molar ratios, reaction times and pH values. Actually, depending on the operating conditions, it was possible to detect variable amounts of 2,6-dimethoxy-1,4-benzoquinone (DMBQ), a highly genotoxic compound, but no N-nitrosoderivative. The highest conversion of DMP into DMBQ was obtained when concentrated acidic solutions of DMP and NaNO2 (molar ratio 1:1.9) reacted at pH 3.0-4.0 (50-60% after 1 hour, depending on the pH conditions). When DMP hydrochloride and NaNO2 (molar ratio 1:0.95) were allowed to react at pH 3.5 in a more diluted solution, to mimic gastric conditions, the conversion of DMP into DMBQ after 20 min was about 3%. The breakdown of DMP can be prevented by adding suitable amounts of ascorbic acid to the reagents.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"523-38"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14339672","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
Synthesis and in vitro antibacterial activity of a new series of monobactam derivatives. 新系列单巴坦衍生物的合成及体外抗菌活性研究。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
U Valcavi, R Aveta, A Brandt, G B Corsi, E Bosone, P Farina, G Guazzi
{"title":"Synthesis and in vitro antibacterial activity of a new series of monobactam derivatives.","authors":"U Valcavi,&nbsp;R Aveta,&nbsp;A Brandt,&nbsp;G B Corsi,&nbsp;E Bosone,&nbsp;P Farina,&nbsp;G Guazzi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Using as a model monobactams with a substituted alpha-oxyimino moiety in the side chain (aztreonam), a series of 2-(2-aminothiazol-4-yl)-2-hydrazono-acetamido monobactam (II a, f) were prepared by condensation of the hydrazones (I a, e) (Z form) with tetrabutylammonium 3-amino-4-methyl-2-oxo-1-azetidin-sulphonate. Isomerization occurred during this synthesis and gave the E form of all compounds. Monobactams (II a, f) showed no significant in vitro antibacterial activity when compared with aztreonam and with some cephalosporins bearing the same E-hydrazono side chain.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"559-66"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14338609","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
Synthesis and in vitro antibacterial activity of a new series of monobactam derivatives. 新系列单巴坦衍生物的合成及体外抗菌活性研究。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01 DOI: 10.1002/CHIN.198909182
U. Valcavi, R. Aveta, A. Brandt, G. Corsi, E. Bosone, P. Farina, G. Guazzi
{"title":"Synthesis and in vitro antibacterial activity of a new series of monobactam derivatives.","authors":"U. Valcavi, R. Aveta, A. Brandt, G. Corsi, E. Bosone, P. Farina, G. Guazzi","doi":"10.1002/CHIN.198909182","DOIUrl":"https://doi.org/10.1002/CHIN.198909182","url":null,"abstract":"Using as a model monobactams with a substituted alpha-oxyimino moiety in the side chain (aztreonam), a series of 2-(2-aminothiazol-4-yl)-2-hydrazono-acetamido monobactam (II a, f) were prepared by condensation of the hydrazones (I a, e) (Z form) with tetrabutylammonium 3-amino-4-methyl-2-oxo-1-azetidin-sulphonate. Isomerization occurred during this synthesis and gave the E form of all compounds. Monobactams (II a, f) showed no significant in vitro antibacterial activity when compared with aztreonam and with some cephalosporins bearing the same E-hydrazono side chain.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"135 1","pages":"559-66"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77048640","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
[Antifungal phytoiatric activity of 4-aroylanilides]. [4-芳酰苯胺的抗真菌植物活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
G Massolini, M L Carmellino, A Baruffini
{"title":"[Antifungal phytoiatric activity of 4-aroylanilides].","authors":"G Massolini,&nbsp;M L Carmellino,&nbsp;A Baruffini","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Some N-acylderivatives of 4-aroylanilines were prepared and tested for phytoiatric antimycotic activity. The substances, most unknown, were subjected to in vitro and in vivo tests (in preventive phase). The compounds studied proved to have interesting activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"507-15"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14339667","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
Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones. 5-芳基-6-甲基-4,5-二氢吡啶嗪-3(2H)及相关5-芳基-6-甲基-吡啶嗪-3(2H)的合成及药理研究。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
G A Pinna, M M Curzu, D Barlocco, G Cignarella, E Cavalletti, M Germini, K Berger
{"title":"Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones.","authors":"G A Pinna,&nbsp;M M Curzu,&nbsp;D Barlocco,&nbsp;G Cignarella,&nbsp;E Cavalletti,&nbsp;M Germini,&nbsp;K Berger","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"539-49"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14338605","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
[Synthesis and anti-ulcer activity of 3-arylprop-2-enthionoethyl esters]. [3-芳基丙-2-硫代乙酯的合成及抗溃疡活性]。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
F Guerrera, M C Sarvà, M A Siracusa, G Ronsisvalle, G Conforto, S Dibennardo, G Failla, M Matera
{"title":"[Synthesis and anti-ulcer activity of 3-arylprop-2-enthionoethyl esters].","authors":"F Guerrera,&nbsp;M C Sarvà,&nbsp;M A Siracusa,&nbsp;G Ronsisvalle,&nbsp;G Conforto,&nbsp;S Dibennardo,&nbsp;G Failla,&nbsp;M Matera","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of 3-arylprop-2-enthionoester derivatives was synthesized. These compounds were evaluated for their antiulcer activity. Derivatives [(H), (V), (VIII)] showed a noteworthy activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"551-8"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14338607","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
Synthesis of some derivatives of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(piperazin-1-yl)-3-quino linecarbo xylic acid (norfloxacin) as potential antibacterial agents. 1-乙基-6-氟-1,4-二氢-4-氧-7-(哌嗪-1-基)-3-喹诺线羧酸(诺氟沙星)衍生物的合成。
Il Farmaco; edizione scientifica Pub Date : 1988-06-01
M Pappalardo, A Omodei-Salè, G Zanuso, A Gutierrez, L Moujir, F G De Las Heras
{"title":"Synthesis of some derivatives of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(piperazin-1-yl)-3-quino linecarbo xylic acid (norfloxacin) as potential antibacterial agents.","authors":"M Pappalardo,&nbsp;A Omodei-Salè,&nbsp;G Zanuso,&nbsp;A Gutierrez,&nbsp;L Moujir,&nbsp;F G De Las Heras","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Twelve new fluoroquinolones, structurally related to norfloxacin, have been synthesized in order to investigate the effect of substituents at the secondary nitrogen of the piperazine ring on antimicrobial activity. The new substances (carbamates, isoureas, guanidines, ureas and cyanamides) tested on a variety of gram-positive and gram-negative organisms showed lower activity than the model compound.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"489-99"},"PeriodicalIF":0.0,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14339665","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
[Dihydro-5,6-imidazo[2,1-b]thiazoles, dihydro-2,3-imidazo[2,1-b]benzothiazoles, analogs of levamisole]. 苯丙胺类兴奋剂[2g—b]
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
H Amarouch, P R Loiseau, M Bonnafous, R Caujolle, M Payard, P M Loiseau, C Bories, P Gayral
{"title":"[Dihydro-5,6-imidazo[2,1-b]thiazoles, dihydro-2,3-imidazo[2,1-b]benzothiazoles, analogs of levamisole].","authors":"H Amarouch,&nbsp;P R Loiseau,&nbsp;M Bonnafous,&nbsp;R Caujolle,&nbsp;M Payard,&nbsp;P M Loiseau,&nbsp;C Bories,&nbsp;P Gayral","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>New compounds containing 5,6-dihydro imidazo[2,1-b]thiazole, 2,3,5,6-tetrahydro imidazo[2,1-b]thiazole and 2,3-dihydro imidazo[2,1-b]benzothiazole rings, substituted by heterocycles analogue to chromones, were synthesized and screened against three nematodes, in vitro. The results indicate moderate anthelmintic properties, compared to levamisole; nevertheless, some products exhibit a significant degree of activity.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"421-37"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14348569","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
[Analysis of the correlation between hydrophilic-lipophilic balance, coefficient of diffusion and hydrogen ion concentration in a series of nonsteroidal anti-inflammatory drugs]. [一系列非甾体类抗炎药亲水亲脂平衡、扩散系数与氢离子浓度的相关性分析]。
Il Farmaco; edizione scientifica Pub Date : 1988-05-01
M I La Rotonda, B Cappello, M Grimaldi, C Silipo, A Vittoria
{"title":"[Analysis of the correlation between hydrophilic-lipophilic balance, coefficient of diffusion and hydrogen ion concentration in a series of nonsteroidal anti-inflammatory drugs].","authors":"M I La Rotonda,&nbsp;B Cappello,&nbsp;M Grimaldi,&nbsp;C Silipo,&nbsp;A Vittoria","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A thorough investigation on the dependence of rate diffusion constants (Kd) of nonsteroidal antiinflammatory drugs on pH and pKa values was carried out. It is shown that a modified multiparametric curve-fitting technique may constitute an useful tool to describe the rate diffusion pH-profiles of ionogenic substances. A comparison between the Kd values and the corresponding distribution coefficients (log D) shows that these constants identify complementary parameters very useful in the study of structure-activity relationships of ionogenic substances.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 5","pages":"439-55"},"PeriodicalIF":0.0,"publicationDate":"1988-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"14348570","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
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