Farmaco (Societa chimica italiana : 1989)最新文献_第6页

Synthesis, biological and modeling studies of 1,3-di-n-propyl-2,4-dioxo-6-methyl-8-(substituted) 1,2,3,4-tetrahydro [1,2,4]-triazolo [3,4-f]-purines as adenosine receptor antagonists 1,3-二-正丙基-2,4-二氧基-6-甲基-8-(取代)1,2,3,4-四氢[1,2,4]-三唑[3,4-f]-嘌呤作为腺苷受体拮抗剂的合成、生物学和模型研究

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-08-01 DOI: 10.1016/j.farmac.2005.04.012

G. Pastorin , C. Bolcato , B. Cacciari , S. Kachler , K.-N. Klotz , C. Montopoli , S. Moro , G. Spalluto

{"title":"Synthesis, biological and modeling studies of 1,3-di-n-propyl-2,4-dioxo-6-methyl-8-(substituted) 1,2,3,4-tetrahydro [1,2,4]-triazolo [3,4-f]-purines as adenosine receptor antagonists","authors":"G. Pastorin , C. Bolcato , B. Cacciari , S. Kachler , K.-N. Klotz , C. Montopoli , S. Moro , G. Spalluto","doi":"10.1016/j.farmac.2005.04.012","DOIUrl":"10.1016/j.farmac.2005.04.012","url":null,"abstract":"<div>A new series of potential adenosine receptor antagonists with a [1,2,4]-triazolo-[3,4-f]-purine structure bearing at the 1 and 3 position n-propyl groups have been synthesized, and their affinities at the four human adenosine receptor subtypes (A1, A2A, A2B and A3) have been evaluated. In this case the presence of n-propyl groups seems to induce potency at the A2A and A3 adenosine receptor subtypes as opposed to our previously reported series bearing methyl substituents at the 1 and 3 positions. In particular the non-acylated derivative 17 showed affinity at these two receptor subtypes in the micromolar range. Indeed, preliminary molecular modeling investigations according to the experimental binding data indicate a modest steric and electrostatic antagonist-receptor complementarity.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 8","pages":"Pages 643-651"},"PeriodicalIF":0.0,"publicationDate":"2005-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.012","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25140499","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

Quantitative analysis of bucillamine and its pharmaceutical formulation using FT-IR spectroscopy 傅里叶红外光谱法定量分析布吉拉胺及其制剂

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-08-01 DOI: 10.1016/j.farmac.2005.05.008

Andrei A. Bunaciu , Hassan Y. Aboul-Enein , Şerban Fleschin

引用次数: 7

High performance liquid chromatographic determination of oxeladin citrate and oxybutynin hydrochloride and their degradation products 高效液相色谱法测定枸橼酸奥拉西丁和盐酸奥施布宁及其降解产物

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-08-01 DOI: 10.1016/j.farmac.2005.06.001

Alaa El-Gindy

{"title":"High performance liquid chromatographic determination of oxeladin citrate and oxybutynin hydrochloride and their degradation products","authors":"Alaa El-Gindy","doi":"10.1016/j.farmac.2005.06.001","DOIUrl":"10.1016/j.farmac.2005.06.001","url":null,"abstract":"<div>Two high performance liquid chromatographic (HPLC) methods are presented for the determination of oxeladin citrate (OL) and oxybutynin hydrochloride (OB) and their degradation products. The first method was based on HPLC separation of OL from its degradation product using a Nucleosil C18 column with a mobile phase consisting of acetonitrile –0.1% phosphoric acid (60:40 v/v). The second method was based on HPLC separation of OB from its degradation product using a VP-ODS C18 column with a mobile phase consisting of acetonitrile/0.01 M potassium dihydrogen phosphate/diethylamine (60:40:0.2). Quantitation was achieved with UV detection at 220 nm based on peak area. The two HPLC methods were applied for the determination of OL or OB, their degradation products, methylparaben and propylparaben in pharmaceutical preparations. The proposed methods were used to investigate the kinetics of acidic and alkaline degradation processes of OL and OB at different temperatures and the apparent pseudofirst-order rate constant, half-life and activation energy were calculated. The pH-rate profiles of degradation of OL and OB in Britton–Robinson buffer solutions within the pH range 2–12 were studied.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 8","pages":"Pages 689-699"},"PeriodicalIF":0.0,"publicationDate":"2005-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.06.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24903460","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

Preparation and phase behaviour of surface-active pharmaceuticals: self-assembly of DNA and surfactants with membranes. Differential adiabatic scanning microcalorimetric study 表面活性药物的制备和相行为:DNA和表面活性剂与膜的自组装。差示绝热扫描微量热研究

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-08-01 DOI: 10.1016/j.farmac.2005.05.010

Erhan Süleymanoğlu

{"title":"Preparation and phase behaviour of surface-active pharmaceuticals: self-assembly of DNA and surfactants with membranes. Differential adiabatic scanning microcalorimetric study","authors":"Erhan Süleymanoğlu","doi":"10.1016/j.farmac.2005.05.010","DOIUrl":"10.1016/j.farmac.2005.05.010","url":null,"abstract":"<div>Some energetics issues relevant to preparation and surface characterization of zwitterionic phospholipid–DNA self-assemblies, as alternative models of the currently used problematic lipoplexes are presented. Nucleic acid compaction capacities of Mg2+ and N-alkyl-N,N,N-trimetylammonium ions (CnTMA, n  12) were compared, with regard to surface interaction with unilamellar vesicles. Differential adiabatic scanning microcalorimetric measurements of synthetic phosphatidylcholine liposomes and calf thymus DNA and their ternary complexes with Mg2+ and C12TMA, were employed for deduction of the thermodynamic model describing their structural transitions. Small monodisperce and highly stable complexes are established after precompaction of DNA with detergent, followed by addition of liposomes. In contrast, divalent metal cation-mediated aggregation of vesicles either leads to heterogeneous multilamellar DNA–lipid arrangements, or to DNA-induced bilayer destabilization and lipid fusion. Possible dependence of the cellular internalization and gene transfection efficiency on the structure and physicochemical properties of DNA–Mg2+–liposomes or DNA–cationic surfactant–liposome systems is emphasized by proposing the structure of their molecular self-organizations with further implications in gene transfer research.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 8","pages":"Pages 701-710"},"PeriodicalIF":0.0,"publicationDate":"2005-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24903463","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

Influence of synthesis and processing conditions on the release behavior and stability of sol–gel derived silica xerogels embedded with bioactive compounds 合成和加工条件对包埋生物活性化合物的溶胶-凝胶衍生二氧化硅干凝胶释放行为和稳定性的影响

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-08-01 DOI: 10.1016/j.farmac.2005.05.007

M. Morpurgo , D. Teoli , B. Palazzo , E. Bergamin , N. Realdon , M. Guglielmi

{"title":"Influence of synthesis and processing conditions on the release behavior and stability of sol–gel derived silica xerogels embedded with bioactive compounds","authors":"M. Morpurgo , D. Teoli , B. Palazzo , E. Bergamin , N. Realdon , M. Guglielmi","doi":"10.1016/j.farmac.2005.05.007","DOIUrl":"10.1016/j.farmac.2005.05.007","url":null,"abstract":"<div>The influence of processing parameters and synthetic strategies in the properties of sol–gel derived silica matrices intended for the release of bioactive compounds was investigated. The time-evolution of the matrix properties during its aging at room temperature in the dry and wet forms was investigated by measuring some of its physical and drug retaining properties. The results indicate that long term gel aging in the wet form is fundamental for the obtainment of dry matrices that are stable upon storage, a fundamental requirement for any practical application. In the case of hybrid matrices obtained by replacing part of the tetraethoxysilane precursor with mono-methyl trimethoxysilane, the order of addition of the reaction component is also important in determining the properties of the final dry gel, probably by influencing the polymer structural properties. This parameter acts synergistically with the matrix composition in determining the release properties of xerogels embedded with bioactive compounds.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 8","pages":"Pages 675-683"},"PeriodicalIF":0.0,"publicationDate":"2005-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.007","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25157185","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: 15

Adsorptive stripping voltammetric determination of triprolidine hydrochloride in pharmaceutical tablets 吸附溶出伏安法测定片剂中盐酸曲普利定的含量

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.05.003

S.I.M. Zayed , I.H.I. Habib

{"title":"Adsorptive stripping voltammetric determination of triprolidine hydrochloride in pharmaceutical tablets","authors":"S.I.M. Zayed , I.H.I. Habib","doi":"10.1016/j.farmac.2005.05.003","DOIUrl":"10.1016/j.farmac.2005.05.003","url":null,"abstract":"<div>The electrochemical behavior of antihistaminic drug, viz. triprolidine hydrochloride (TripCl), at a hanging mercury drop electrode (HMDE) is investigated. Chemical and electrical parameters affecting the adsorptive voltammetric measurements are optimized. Different modes of sweep, viz. direct current DC, normal pulse NP, differential pulse DP and square wave SW modes, over the potential range from –800 to –1400 mV, are used in the presence of 0.04 M Britton–Robinson buffer pH 11, with accumulation time 30 s, scan rate 50 mV/s and pulse amplitude 50 mV. The reduction process is irreversible and involved the transfer of two electrons and two protons. Their responses are linear over the concentration range 15–157 ng/ml with average correlation coefficient 0.9998, while the detection limit is 2.64, 6.24, 8.80 and 2.12 ng/ml for DC, DP, SW and NP mode, respectively. The differential pulse method has been applied successfully for the determination of the drug in Egyptian pharmaceutical preparation with mean recovery 99.55  <!-->0.67%.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 621-625"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25304415","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: 8

Synthesis and antibacterial activity of 1H-pyrazolo[3,4-b]pyrazine and -pyridine derivatives 1h -吡唑[3,4-b]吡嗪及-吡啶衍生物的合成及抑菌活性研究

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.05.002

Henryk Foks , Danuta Pancechowska-Ksepko , Anna Kędzia , Zofia Zwolska , Mieczysław Janowiec , Ewa Augustynowicz-Kopeć

{"title":"Synthesis and antibacterial activity of 1H-pyrazolo[3,4-b]pyrazine and -pyridine derivatives","authors":"Henryk Foks , Danuta Pancechowska-Ksepko , Anna Kędzia , Zofia Zwolska , Mieczysław Janowiec , Ewa Augustynowicz-Kopeć","doi":"10.1016/j.farmac.2005.05.002","DOIUrl":"10.1016/j.farmac.2005.05.002","url":null,"abstract":"<div>The investigations of new pyrazine and pyridine derivatives showing an antibacterial activity have been made. Upon treatment of 3-chloro-2-cyanopyrazine [1] and 2-chloro-3-cyanopyridine with 1,1-dimethyl-hydrazine, 1-aminopiperidine and 1-amino-4-methylpiperazine, either the pyrazolo-pyrazine (1), and -pyridine (2) derivatives, or ammonium salts (3–8) were obtained, according to the reaction conditions. Compound 1 was obtained in the reaction of the initial nitrile with methylhydrazine as well. The reactions of 1 gave the following derivatives: acylation—(9), that with p-chlorobenzoic aldehyde—(10), and with phenyl-isothiocyanate—(11). 3-Chloro-2-cyanopyrazine treated with hydrazine hydrate gave amidrazone (12), which upon condensation with p-chlorobenzoic aldehyde produced (13). The compounds obtained were tested in vitro for their tuberculostatic activity. The minimal inhibitory concentration (MIC) values were within 22–100 μg/cm3. Compounds 1, 5 and 6 were also tested in vitro for their activity towards 25 strains of anaerobic, and 25 strains of aerobic bacteria. They appeared to be of elevated activity towards the anaerobes and of low one towards the aerobes (Table 2).</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 513-517"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25304418","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: 76

HPLC determination of certain flavonoids and terpene lactones in selected Ginkgo biloba L. phytopharmaceuticals 高效液相色谱法测定银杏植物药中黄酮类和萜烯内酯的含量

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.01.014

Mostafa K. Mesbah , Sherief I. Khalifa , Alaa El-Gindy , Kamilia A. Tawfik

引用次数: 37

Study on the inclusion complex between β-cyclodextrin and celecoxib by spectrofluorimetry and its analytical application 用荧光光谱法研究β-环糊精与塞来昔布的包合物及其分析应用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.02.003

Jamshid L. Manzoori, Hossein Abdolmohammad-Zadeh, Mohammad Amjadi

{"title":"Study on the inclusion complex between β-cyclodextrin and celecoxib by spectrofluorimetry and its analytical application","authors":"Jamshid L. Manzoori, Hossein Abdolmohammad-Zadeh, Mohammad Amjadi","doi":"10.1016/j.farmac.2005.02.003","DOIUrl":"10.1016/j.farmac.2005.02.003","url":null,"abstract":"<div>The supramolecular interaction of celecoxib (chemically 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamide) and β-cyclodextrin (β-CD) has been studied by spectrofluorimetry. The results showed that β-CD reacted with celecoxib to form an inclusion complex. 1:1 stoichiometry for β-CD-celecoxib complex was established and its association constant at different temperatures was calculated by applying a non-linear regression method to the change in the fluorescence of celecoxib that brought about by the presence of β-CD. The thermodynamic parameters (ΔH°, ΔS° and ΔG°) associated with the inclusion process were also determined. Based on the significant enhancement of the fluorescence intensity of celecoxib produced through complex formation, a simple, rapid and highly sensitive spectrofluorimetric method for the determination of celecoxib in aqueous solution in the presence of β-CD was developed. The measurement of relative fluorescence intensity was carried out at 390 nm with excitation at 270 nm. A linear relationship between the fluorescence intensity and celecoxib concentration was obtained in the range of 0.1–4.0 μg ml–1, with a correlation coefficient of 0.9996. The detection limit was 7.29 ng ml–1 and the relative standard deviation was 1.28%. The method was successfully applied to the determination of celecoxib in pharmaceutical preparations.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 575-581"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.02.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40939012","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

Metabolic effects of novel N-1-sulfonylpyrimidine derivatives on human colon carcinoma cells 新型n -1磺酰基嘧啶衍生物对人结肠癌细胞的代谢作用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.006

Ljubica Glavaš-Obrovac , Ivan Karner , Mario Štefanić , Jelena Kašnar-Šamprec , Biserka Žinić

{"title":"Metabolic effects of novel N-1-sulfonylpyrimidine derivatives on human colon carcinoma cells","authors":"Ljubica Glavaš-Obrovac , Ivan Karner , Mario Štefanić , Jelena Kašnar-Šamprec , Biserka Žinić","doi":"10.1016/j.farmac.2005.04.006","DOIUrl":"10.1016/j.farmac.2005.04.006","url":null,"abstract":"<div>Novel N-1-sulfonylpyrimidine derivatives have a strong antiproliferative activity and an ability to induce apoptosis in treated tumor cells. The purpose of this study was to elucidate the effects of two N-1-sulfonylpyrimidine nucleobases on catalytic activity of tumor cells' enzymes involved in DNA and RNA synthesis, and in de novo and salvage pyrimidine and purine syntheses. Investigations were performed in vitro on colon carcinoma cells (Caco2). The biosynthetic activity of the tumor cells' enzymes was determined using sensitive radio-assays. Enzyme activity in treated cells was calculated relative to untreated control cells. Both of the investigated compounds, 1-(p-toluenesulfonyl) cytosine (TsC) and 5-bromo-1-(methanesulfonyl) uracil (BMsU) inhibited activities of specific enzymes involved in nucleic acid synthesis. BMsU strongly inhibited activities of DNA polymerase α (53%), thymidine kinase (68%), thymidilate synthase (43%), and ribonucleotide reductase (46%). De novo biosynthesis of pyrimidine and purine was reduced by 20%. TsC was able to inhibit RNA polymerase (37%), orotate phosphoribosyltransferase (39%), uridine kinase (44%), ribonucleotid reductase (47%), and de novo purine synthesis (61%). Antitumor activity of 1-(p-toluenesulfonyl) cytosine (TsC) and 5-bromo-1-(methanesulfonyl) uracil (BMsU) is closely associated with their inhibitory activity on enzymes that play an important role in the metabolism of tumor cells.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 479-483"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40928310","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: 11