Bollettino chimico farmaceutico最新文献

{"title":"Synthesis and fungicidal activity of some 5-aryl/aryloxymethyl-2-[5-aryl-3-methyl-1,2,4-triazol-2-yl]-1,3,4-thiadiazoles and 5-aryl/aryloxymethyl-2[5-aryl-2-phenylimino-1,3,4- thiadiazolin-3-yl]-1,3,4-thiadiazoles.","authors":"Nizamuddin,&nbsp;K Begum,&nbsp;M K Srivastav,&nbsp;M Hussain Khan","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>5-Aryl/aryloxymethyl-2-[5-aryl-2-methyl-1,2,4-triazol-2-yl]- 1,3,4-thiadiaxoles 4 and 5-Aryl/aryloxymethyl-2-[5-aryl-2-phenylimino-1,3,4- thiadiazolin-3-yl]-1,3,4-thiadiazoles 5 have been obtained from the cyclocondensation of 5-aryl/aryloxymethyl-2-arylidene hydrazino-1,3,4-thiadiazoles 3 with methyl cyanide and phenyl isothiocyanate respectively. Compounds 4 & 5 have been screened for their fungicidal activity against R. solani, F. oxysporum and P. oryzae. Based on screening data some structure-activity relationship is given.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"420-5"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400758","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}

{"title":"Pyrimidines. Part II: Synthesis of novel pyrimidines, 1,2,4-triazolo[4,3-a]pyrimidin-7-ones and pyrimidino[2,1-c][1,2,4]triazin-8-ones for their antimicrobial and anticancer activities.","authors":"N S Habib,&nbsp;R Soliman,&nbsp;K Ismail,&nbsp;A M Hassan,&nbsp;M T Sarg","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Five main classes of novel pyrimidine derivatives have been synthesized; namely 6-substituted phenyl-5-cyano-3-methyl-2-phenacylhydrazino-3,4-dihydropyrimidin-4-ones 4a-e; 6-substituted phenyl-2-arylidene hydra-zino-5-cyano-3-methyl-3,4-dihydropyrimidin-4-ones 5a-i; 6-substituted phenyl-2-acylhydrazino-5-cyano-3-methyl-3,4-dihydropyrimidin-4-ones 7a-d, 8a-e and 9a-c; three novel series of 1,2,4-triazolo[4,3-a] pyrimidones 10a,b, 11a-d and 12a-d and 6-substituted phenyl-7-cyano-9-methyl-3-phenyl or 4-chlorophenyl-4,9-dihydropyrimido[2,1-c][1,2,4] triazin-8-ones 13a-c. Besides, the azide compound 2-azido-5-cyano-3-methyl-6-phenyl-3,4-dihydropyrimidin-4-one 6 was also synthesized. The prepared compounds were tested for antimicrobial and anticancer activity. Compounds 4b and 4d showed promising activity against Escherichia coli. Compounds 3c, 5c, 5e, 5g and 7b were active in the three cell line antitumor one dose primary assay and were evaluated in the 60 human tumor full panel cell line invitro screening. Compound 5c showed promising activity against all types of leukemia especially leukemia K-562 and leukemia SR with GI50 = 1.61 and 2.63 mmol/l respectively.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"396-405"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400189","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}

{"title":"The positive way of thinking and the acquaporines.","authors":"G C Lubner","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"378"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400252","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}

{"title":"Purification and some properties of African oil bean seed lipoxygenase--Part 1.","authors":"M N Anokwulu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Lipoxygenase was extracted from African oil bean seed and purified by ammonium sulphate precipitation, gel filtration on Sephadex G-25 and ion-exchange chromatography on DEAE--cellulose column. The enzyme was purified 79.63 fold and 36% of the enzyme activity was recovered. The molecular weight of the enzyme was 102,000 daltons and the peroxide value was 10.56 x 10(-3) mM. The Vmax was 0.14 OD min-1 while the Km value was 1.92 x 10(-4) M. The enzyme had an optimum pH of 7.0 and optimum temperature of 30 degrees C. While diethyl-dithiocarbamate was the best inhibitor of the enzyme's oxidation of linoleic acid, nordihydroguiaretic acid was the best antioxidant for its oxidation of the fatty acid. African oil bean seed lipoxygenase had high enzyme activity of 86% when compared to soybean lipoxygenase (considered to be the best source of the enzyme). This means that African oil bean seed is a good source of lipoxygenase for biotechnology such as the bleaching of browned yam tubers.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"410-5"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400756","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}

{"title":"Synthesis of some new thiazole derivatives of pharmaceutical interest.","authors":"Fawzia Zakeria el-Ablack","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Reaction of 4-amino-3-phenyl-5-ethoxycarbonyl-thiazole-2-thione with phenylisothiocyanate gave (2) which when boiled with acetic acid gave (3). Treatment of (2) with monochloroacetic acid resulted in the formation of thiazolidinone derivative (4). Reaction of (2) with malonic acid gave (5). Condensation of (1) with aromatic aldehydes afforded Schiffe base derivatives (6a,b). Treatment of (1) with malononitrile, ethyl cyanoacetate and acetonitrile resulted the formation of pyridine derivatives (7a,b,c). The reaction of (1) with urea and thiourea gave compound (8). Condensation of (1) with o-phenylenediamine and o-aminophenol gave compound (9). Reaction of (1) with nitrous acid followed by coupling with ethylacetoacetate afforded (10). Bromination of (10) gave bromo derivative (11). The structures of the hitherto unknown compounds have been confirmed by analytical and spectral methods. The newly synthesized compounds were screened for antibacterial activity.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 9","pages":"406-9"},"PeriodicalIF":0.0,"publicationDate":"2003-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24400191","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}

{"title":"Studies of wet granulation in small scale high shear mixer of 20 mg tablets of policosanol.","authors":"E Uribarri,&nbsp;A Laguna,&nbsp;M González","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>It was studied the influence of three factors in the manufacturing process of tablets containing 20 mg of policosanol in a small scale when was used a high shear mixer. A factorial design without repetitions was used, considering as independent variables: volume of binder solution, kneading time and the use or not of chopper. Data analysis was carried out using the Yates algorithm, considering the effect of these three factors over the diameter of the granules, the percent of fine powders in granulate and the compression forces. The diameter of the granules was increased with an increase in the volume of the binder solution added and with an increase in the kneading time and was decreased when the chopper was used. The percent of fine powders, present in granulate, was significantly diminished with an increase of the volume of binder solution and diminished with an increase in the kneading time, the influence of the use of chopper was insignificant. The compression forces diminished with the use of chopper, with the increase of the volume of binder solution used and are not affected with the changes in the kneading time.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 8","pages":"343-6"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40858779","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}

{"title":"O/W microemulsions for oral drug delivery.","authors":"A Carlucci,&nbsp;M Cicconi Vidal,&nbsp;R García,&nbsp;C Bregni","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Quaternary microemulsion compositions for oral administration using isopropyl myristate, polysorbate 80 and ethanol 96 degrees were developed and three ratio of polysorbate to ethanol were selected. Isotropic single-phase compositions were considered as microemulsions and were registered on a Pseudo-Ternary Phase Diagram. The objective was to formulate a therapeutic dose for lorazepam and loperamide in a drop liquid form. Another aim was to obtain a liquid oral formula for nifedipine taking advantage of its insured fast absorption to be used in hypertensive crises. The physical stability of the compositions was evaluated by normal aging, centrifugal resistance time and by cycling as well. The selected formulation characterization included density, pH and conductivity measurements. The particle size distribution was determined by a light scattering method and, finally the carried drugs concentration was valued. The versatility showed by this type of systems allows both to carry drugs of different physico-chemical properties and to deal with a number of pharmacotherapeutic objectives.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 8","pages":"324-9"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40936078","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}

{"title":"Influence of polymers weight ratio and pH of polymers solution on the characteristics of chitosan-carboxymethyl cellulose microspheres containing theophylline.","authors":"M A Bayomi","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Optimization of formulation for chitosan-carboxymethyl cellulose (CH-CMC) microspheres that contain a drug of narrrow therapeutic index was the interest of this study. Theophylline (TPH) was chosen as a model drug. The effects of chitosan:sodium carboxymethyl cellulose (CH:SCMC) weight ratio (X1) and pH of polymers solution (X2) as independent variables on the physical characteristics of the microspheres as well as release profile of TPH from microspheres prepared by the emulsion coacervation-phase separation technique were studied. The influence of each of the two variables on responses such as angle of repose, compressibility index, incorporation efficiency particle size, initial drug release, time for 50% drug release (T50%) and % drug released in 8 hours was investigated. Generally, the increase in CH:SCMC weight ratio showed to increase the incorporation efficiency of the drug, increase the particle size and decrease the flowability of the microspheres. The increase of CH:SCMC ratio was also responsible to get low initial drug release, slow drug release (long T50%) and incomplete total drug released in 8 hours. On the other hand, high and low pHs of polymers solution were responsible to decrease drug incorporation in the microspheres and to produce small particles while, good flowability was obtained at pHs 2.5 and 4. A full factorial experimental design was employed to investigate the effect of the two independent variables on the responses. The results were analyzed by a general quadratic equation and response surfaces generated. From the obtained regression, it was concluded that the effect of CH:SCMC polymers ratio is more significant in changing the values of flowability particle size and drug release in 8 hours while pH values were more significant in changing the values of initial drug release and T50%. On the other hand the interaction coefficients of the two variables showed synergistic effect on flowability and drug release in 8 hours while, there were antagonist effects on particle sizes and T50%. From the optimization studies it is possible to choose the conditions required for the preparation of microspheres with the desired characteristics.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 8","pages":"336-42"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40858778","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}

{"title":"The Italian way to nanotherapies.","authors":"G C Lubner","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 8","pages":"310"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40936074","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}

{"title":"Optimal conditions for accumulation of bioavailable iron in Saccharomyces cerevisiae cells.","authors":"L Gligic,&nbsp;N Vujovic,&nbsp;B Stevovic,&nbsp;J Manic","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Growth and proliferation of brewer's yeast Saccharomyces cerevisiae in the presence of different Fe2+ levels was studied with the aim of finding optimal conditions for a maximum accumulation of bioavailable iron bound to constituents of yeast cells. The results demonstrated that iron stimulates growth and proliferation only under conditions of intensive aeration. Iron accumulation and the effect of aeration were examined in the presence 3.6 microM - 7.2 mM Fe2+, while its content in the cells after 20 h cultivation was determined by atomic absorption spectrophotometry. Control cultures were grown in no iron added medium. Further experiments revealed that iron concentrations ranging from 3.6 microM to 3.6 mM were beneficial to growth and proliferation, while higher levels did not affect these processes. The above range of iron concentrations also led to a more extensive iron accumulation, while further increase expressed no effect. So, Fe2+ concentration of 3.6 mM, enabling its high accumulation within the cells, while not negatively affecting biomass yield was selected for further studies. Iron uptake led to the modifications in transport of several other elements (Ca2+, Zn2+, K+ and Na+) and thus to the change in ion composition of the cells in comparison with the corresponding control.</p>","PeriodicalId":9085,"journal":{"name":"Bollettino chimico farmaceutico","volume":"142 8","pages":"330-2"},"PeriodicalIF":0.0,"publicationDate":"2003-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40936079","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}