Farmaco (Societa chimica italiana : 1989)最新文献_第8页

Development and validation of a procedure for the determination of minoxidil in hair-regrowth formulations using two variants of capillary zone electrophoresis 用两种毛细管区带电泳法测定毛发再生制剂中米诺地尔含量的方法的建立和验证

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.002

S.C. Patterson , T. Ramstad , K.A. Mills

引用次数: 14

Voltammetric determination of montelukast sodium in dosage forms and human plasma 孟鲁司特钠剂型和人血浆的伏安法测定

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.004

I. Alsarra , M. Al-Omar , E.A. Gadkariem , F. Belal

{"title":"Voltammetric determination of montelukast sodium in dosage forms and human plasma","authors":"I. Alsarra , M. Al-Omar , E.A. Gadkariem , F. Belal","doi":"10.1016/j.farmac.2005.04.004","DOIUrl":"10.1016/j.farmac.2005.04.004","url":null,"abstract":"<div>The voltammetric behaviour of montelukast (MKST) was studied using cyclic voltammetry, direct current (DCt), differential pulse polarography (DPP) and alternating current (ACt) polarography. MKST exhibited well-defined cathodic waves over the range pH range 1–5. No anodic waves were produced over the same pH range. At pH 1, the analytical pH; the diffusion current constant (Id) was 2.2±0.01 μA l mmol–1. The current concentration plot was rectilinear over the range 2–20 μg ml–1 with correlation coefficient (n    =5) was 101.38±3.85. The number of electrons transferred in the reduction process could be accomplished and a proposal of the electrode reaction was proposed.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 563-567"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40938973","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: 44

Synthesis and anti-tyrosine kinase activity of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives: investigation of their role against p60c-Src receptor tyrosine kinase with the application of receptor docking studies 3-(取代苄基)- 1,3 -二氢吲哚啉衍生物的合成及抗酪氨酸激酶活性:应用受体对接研究其对p60c-Src受体酪氨酸激酶的作用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.01.015

Sureyya Olgen , Eiichi Akaho , Dogu Nebioglu

{"title":"Synthesis and anti-tyrosine kinase activity of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives: investigation of their role against p60c-Src receptor tyrosine kinase with the application of receptor docking studies","authors":"Sureyya Olgen , Eiichi Akaho , Dogu Nebioglu","doi":"10.1016/j.farmac.2005.01.015","DOIUrl":"10.1016/j.farmac.2005.01.015","url":null,"abstract":"<div>A series of 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-thione derivatives were synthesized as modified congeners of 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one series. All the synthesized compounds were examined for their in vitro anti-tyrosine kinase activity against p60c-Src. The activity results revealed that compounds (Z)-3-(4′-Dimethylamino-benzylidene)-1, 3-dihydro-indolin-2-thione (12) (E)-3-(2′, 6′-Dichloro-benzylidene)-1, 3-dihydro-indolin-2-thione (13) and (E)-3-(3′-Hydroxy-4′-methoxy-benzylidene)-1, 3-dihydro-indolin-2-thione (19) exhibited anti-tyrosine kinase activity with IC50 value of 21.91, 21.20 and 30.92 μM, respectively. These results are comparable to PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3, 4-d]pyrimidine-4-yl-amine] (IC50  <!-->0.17 μM), which is reported as a potent and selective p60c-Src tyrosine kinase inhibitor. Some thio congeners are found to be more potent than oxo derivatives; however, no significant correlation was observed between the activity profiles of these two series. Docking program was used to investigate the docking mode of each compound at the active site. Among all of the compounds, only (Z)-3-(2′-Chloro-benzylidene)-1, 3-dihydro-indolin-2-one (8) and (E)-3-(3′-Nitro-benzylidene)-1, 3-dihydro-indolin-2-thione (16) were docked at the active site where the PP1 was embedded.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 497-506"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.01.015","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40939717","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: 28

Determination of isoxsuprine hydrochloride by sequential injection visible spectrophotometry 顺序注射可见分光光度法测定盐酸异苏嘌呤的含量

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.05.001

Negussie W. Beyene , Jacobus F. Van Staden , Raluca-Ioana Stefan , Hassan Y. Aboul-Enein

{"title":"Determination of isoxsuprine hydrochloride by sequential injection visible spectrophotometry","authors":"Negussie W. Beyene , Jacobus F. Van Staden , Raluca-Ioana Stefan , Hassan Y. Aboul-Enein","doi":"10.1016/j.farmac.2005.05.001","DOIUrl":"10.1016/j.farmac.2005.05.001","url":null,"abstract":"<div>An automated sequential injection (SI) spectrophotometric method for the determination of isoxsuprine hydrochloride is described. The method is based on the condensation of aminoantipyrine with phenols (isoxsuprine hydrochloride) in the presence of an alkaline oxidizing agent (potassium hexacyanoferrate) to yield a pink colored product, the absorbance of which is monitored at 507 nm. Chemical as well as physical SI parameters that affect the signal response have been optimized in order to get better sensitivity, higher sampling rate and better reagent economy. Using the optimized aforesaid parameters, a linear relationship between the relative peak height and concentration was obtained in the range 1–60 mg l–1. The detection limit (as 3σ value) was 0.3 mg l–1 and precision was 1.4% and 1.6% at 5 and 10 mg l–1, respectively. As compared to previous reports, wide linear range, low detection limit, and highly economical reagent consumption are the advantages of this automated method.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 613-619"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.001","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40946644","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

Nb-benzoyltryptamine derivatives with relaxant activity in guinea-pig ileum 豚鼠回肠中具有松弛活性的nb -苯甲酰色胺衍生物

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.001

Stanley Juan C. Gutierrez , Fladmir de S. Claudino , Bagnólia A. Da Silva , Celso A. Câmara , Reinaldo N. de Almeida , Maria de Fátima V. de Souza , Marcelo S. Da Silva , Emídio V.L. Da-Cunha , José Maria Barbosa-Filho

引用次数: 9

Simple fluorimetric method for determination of certain antiviral drugs via their oxidation with cerium (IV) 铈氧化法测定某些抗病毒药物的简单荧光法(ⅳ)

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.003

Ibrahim A. Darwish , Alaa S. Khedr , Hassan F. Askal , Ramadan M. Mahmoud

{"title":"Simple fluorimetric method for determination of certain antiviral drugs via their oxidation with cerium (IV)","authors":"Ibrahim A. Darwish , Alaa S. Khedr , Hassan F. Askal , Ramadan M. Mahmoud","doi":"10.1016/j.farmac.2005.04.003","DOIUrl":"10.1016/j.farmac.2005.04.003","url":null,"abstract":"<div>A simple and sensitive fluorimetric method for determination of antiviral drugs: ribavirin, acyclovir, and amantadine hydrochloride has been developed. The method was based on the oxidation of these drugs by cerium(IV) in presence of perchloric acid and subsequent monitoring the fluorescence of the induced cerium(III) at λexcitation 255 and λemission 355 nm. Different variables affecting the reaction conditions such as the concentrations of cerium(IV), type and concentration of acid medium, reaction time, temperature, and the diluting solvents were carefully studied and optimized. Under the optimum conditions, linear relationships with good correlation coefficients (0.9978–0.9996) were found between the relative fluorescence intensity and the concentrations of the investigated drugs in the range of 50–1400 ng ml–1. The assay limits of detection and quantitation were 20–49, and 62–160 ng ml–1, respectively. The precision of the method was satisfactory; the values of relative standard deviations did not exceed 1.58%. No interference could be observed from the excipients commonly present in dosage forms. The proposed method was successfully applied to the analysis of the investigated drugs in pure and pharmaceutical dosage forms with good accuracy and precision; the recovery percentages ranged from 99.2 to 101.2±0.48–1.30%. The results obtained by the proposed fluorimetric method were comparable with those obtained by the official method stated in the United States Pharmacopoeia.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 555-562"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.003","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41022195","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: 53

Synthesis and structural characterization of derivatives of 2- and 3-benzo[b]furan carboxylic acids with potential cytotoxic activity 具有潜在细胞毒性活性的2-和3-苯并[b]呋喃羧酸衍生物的合成和结构表征

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.05.005

Jerzy Kossakowski , Kinga Ostrowska , Elżbieta Hejchman , Irena Wolska

{"title":"Synthesis and structural characterization of derivatives of 2- and 3-benzo[b]furan carboxylic acids with potential cytotoxic activity","authors":"Jerzy Kossakowski , Kinga Ostrowska , Elżbieta Hejchman , Irena Wolska","doi":"10.1016/j.farmac.2005.05.005","DOIUrl":"10.1016/j.farmac.2005.05.005","url":null,"abstract":"<div>Derivatives of 2- and 3-benzo[b]furancarboxylic acids were prepared and evaluated for their cytotoxic potential in the National Cancer Institute, Bethesda, USA. Six compounds: 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylic acid (2), 6-hydroxy-7-(p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid (4), 5-bromo-7-hydroxy-6-methoxy-2-benzofurancarboxylic acid methyl ester (6a), 6-acetyl-5-(O-ethyl-2′-diethylamino)-2-methyl-3-benzofurancarboxylic acid methyl ester (1f), 6-(O-ethyl-2′-diethylamino)-7-p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid methyl ester hydrochloride (4b), 5-bromo-7-(O-ethyl-2′-diethylamino)-6-methoxy-2-benzofurancarboxylic acid methyl ester (6b) showed significant cytotoxic activities against human cancer cell lines. In addition the crystal structures of 7-methoxy-2-benzofurancarboxylic acid methyl ester (7a) has been solved by X-ray structure analysis of single crystals.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 519-527"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25132055","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: 26

Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity 具有抗逆转录病毒活性的HIV-1整合酶抑制剂异芳基二酮己烯酸和二酮丁酸的设计、合成和生物学评价

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-05-01 DOI: 10.1016/j.farmac.2005.03.008

R. Di Santo , R. Costi , M. Artico , R. Ragno , G. Greco , E. Novellino , C. Marchand , Y. Pommier

{"title":"Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity","authors":"R. Di Santo , R. Costi , M. Artico , R. Ragno , G. Greco , E. Novellino , C. Marchand , Y. Pommier","doi":"10.1016/j.farmac.2005.03.008","DOIUrl":"10.1016/j.farmac.2005.03.008","url":null,"abstract":"<div>Highly active anti-retroviral therapy (HAART) using reverse transcriptase (RT) and protease (PR) inhibitors and, more recently, inhibitors of the fusion is currently the best clinical approach in combating acquired immunodeficiency syndrome (AIDS), caused by infection from human immunodeficiency virus type 1 (HIV-1). However, this therapy does not completely eradicate the virus, so that resistant strains easily emerge. The above problem calls urgently for research on inhibitors of further viral targets such as integrase (IN), the third enzyme produced by HIV. Recently, our research group was engaged in studies on conformationally restrained cinnamoyl compounds related to curcumin as anti-IN agents. Compounds containing both a 3,4,5-trihydroxyphenyl group and a carboxylic acid function were potent IN inhibitors active against viral replication. More recently, a promising new class of inhibitors synthesized by Merck Company has emerged, which contain aryldiketoacid (ADK) functionality. The ADKs selectively inhibited the stand transfer (ST) step of integration and were proven to be effective IN inhibitors in vivo. Our interest in the field of IN inhibitors led us to designe pyrrole and indole derivatives containing both a cinnamoyl moiety and a diketoacid group. A number of the cited derivatives were proven potent IN inhibitors, which selectively inhibited the ST step at submicromolar concentrations and were effective against virus replication in HIV-1 infected cells.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 5","pages":"Pages 409-417"},"PeriodicalIF":0.0,"publicationDate":"2005-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.03.008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40925879","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: 31

1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII 1,4-和2,4-取代-1,2,3-三唑作为潜在的钾通道活化剂。7

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-05-01 DOI: 10.1016/j.farmac.2005.03.004

Vincenzo Calderone , Irene Giorgi , Oreste Livi , Enrica Martinotti , Alma Martelli , Antonio Nardi

引用次数: 11

Structure–Retention Relationship in a Series of Chiral 1,4-Disubstituted Piperazine Derivatives on Carbohydrate Chiral Stationary Phases 一系列手性1,4-二取代哌嗪衍生物在碳水化合物手性固定相上的结构-保留关系

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-05-01 DOI: 10.1016/j.farmac.2005.01.006

Zdzisław Chilmonczyk , Łukasz Sienicki , Bożena Łozowicka , Małgorzata Lisowska-Kuźmicz , Anna Jończyk , Hassan Y. Aboul-Enein

引用次数: 5