Farmaco (Societa chimica italiana : 1989)最新文献_第7页

Non-imidazole histamine NO-donor H3-antagonists 非咪唑组胺no供体h3拮抗剂

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.007

Paolo Tosco, Massimo Bertinaria, Antonella Di Stilo, Clara Cena, Roberta Fruttero, Alberto Gasco

引用次数: 5

Heterocyclic inhibitors of AChE acylation and peripheral sites 乙酰胆碱酯酰化和外周位点的杂环抑制剂

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.03.010

Maria Laura Bolognesi, Vincenza Andrisano, Manuela Bartolini, Andrea Cavalli, Anna Minarini, Maurizio Recanatini, Michela Rosini, Vincenzo Tumiatti, Carlo Melchiorre

{"title":"Heterocyclic inhibitors of AChE acylation and peripheral sites","authors":"Maria Laura Bolognesi, Vincenza Andrisano, Manuela Bartolini, Andrea Cavalli, Anna Minarini, Maurizio Recanatini, Michela Rosini, Vincenzo Tumiatti, Carlo Melchiorre","doi":"10.1016/j.farmac.2005.03.010","DOIUrl":"10.1016/j.farmac.2005.03.010","url":null,"abstract":"<div><h3>Abstract</h3>Notwithstanding the criticism to the so called “ cholinergic hypothesis”, the therapeutic strategies for the treatment of Alzheimer's disease (AD) have been mainly centered on the restoration of cholinergic functionality and, until the last year, the only drugs licensed for the management of AD were the acetycholinesterase (AChE) inhibitors. Target enzyme AChE consists of a narrow gorge with two separate ligand binding sites: an acylation site at the bottom of the gorge containing the catalytic triad and a peripheral site located at the gorge rim, which encompasses binding sites for allosteric ligands. The aim of this short review is to update the knowledge on heterocyclic AChE inhibitors able to interact with the two sites of enzymes, structurally related to the well known inhibitors physostigmine, rivastigmine and propidium. The therapeutic potential of the dual site inhibithors in inhibiting amyloid-ß aggregatrion and deposition is also briefly summarised.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 465-473"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.03.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25097386","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: 22

A molecular dynamics study of human serum albumin binding sites 人血清白蛋白结合位点的分子动力学研究

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.010

Roberto Artali , Gabriella Bombieri , Luisella Calabi , Antonio Del Pra

{"title":"A molecular dynamics study of human serum albumin binding sites","authors":"Roberto Artali , Gabriella Bombieri , Luisella Calabi , Antonio Del Pra","doi":"10.1016/j.farmac.2005.04.010","DOIUrl":"10.1016/j.farmac.2005.04.010","url":null,"abstract":"<div>A 2.0 ns unrestrained Molecular Dynamics was used to elucidate the geometric and dynamic properties of the HSA binding sites. The structure is not stress affected and the rmsds calculated from the published crystallographic data are almost constant for all the simulation time, with an averaged value of 2.4Å. The major variability is in the C-terminus region. The trajectory analysis of the IIA binding site put in evidence fast oscillations for the Cγ@Leu203···Cγ@Leu275 and Cγ@Leu219···Cγ@Leu260 distances, with fluctuations around 250 ps, 1000 ps and over for the first, while the second is smoothly increasing with the simulation time from 7 to 10Å. These variations are consistent with a volume increase up to 20% confirmed by the inter-domain contacts analysis, in particular for the pair O@Pro148···Oγ@Ser283, representing the change of distance between IB-h9 and IIA-h6, O@Glu149···Oγ@Ser189 for sub-domains IB-h9/IIA-h1 and N@Val339···Oδ2@Asp447 sub-domains IIB-h9/IIIA-h1. These inter-domain motions confirm the flexibility of the unfatted HSA with possible binding site pre-formation.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 485-495"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25132054","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: 66

Application of π-acceptors to the spectrophotometric determination of lisinopril in commercial dosage forms π受体在赖诺普利市售剂型分光光度测定中的应用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.011

Nafisur Rahman, Nishat Anwar, Mohammad Kashif

{"title":"Application of π-acceptors to the spectrophotometric determination of lisinopril in commercial dosage forms","authors":"Nafisur Rahman, Nishat Anwar, Mohammad Kashif","doi":"10.1016/j.farmac.2005.04.011","DOIUrl":"10.1016/j.farmac.2005.04.011","url":null,"abstract":"<div>Two simple, rapid and sensitive spectrophotometric methods have been proposed for the determination of lisinopril in pure form and pharmaceutical formulations. The methods are based on the charge transfer complexation reaction of the drug with 7,7,8,8,tetracyanoquinodimethane (TCNQ) and p-chloranilic acid (pCA) in polar media. The lisinopril–TCNQ and lisinopril–pCA charge transfer complexes dissociate in acetone and methanol, respectively, and yield coloured TCNQ and pCA radical anions which are measured spectrophotometrically at 743 and 525 nm. Under optimised experimental conditions, Beer's law is obeyed in the concentration range of 2–26 and 25–300 μg ml–1 with molar absorptivity of 1.432 × 104 and 1.192 × 104 l mol–1 cm–1 for TCNQ and pCA methods, respectively. Both the methods have been applied to the determination of lisinopril in pharmaceutical dosage forms. Results of analysis are validated statistically.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 605-611"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.011","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40945517","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: 27

Stability of aztreonam in AZACTAM 氮曲仑在AZACTAM中的稳定性

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.009

Marianna Zając , Anna Jelińska , Judyta Cielecka-Piontek , Irena Oszczapowicz

引用次数: 5

Conductimetric determination of phenylpropanolamine HCl, ranitidine HCl, hyoscyamine HBr and betaine HCl in their pure state and pharmaceutical preparations 苯基丙醇胺HCl、雷尼替丁HCl、山莨菪碱HBr、甜菜碱HCl纯态及制剂的电导测定

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.03.002

Yousry M. Issa, Ahmed F.A. Youssef, Ali A. Mutair

引用次数: 18

Linear regression analysis and its application to multivariate chromatographic calibration for the quantitative analysis of two-component mixtures 线性回归分析及其在双组分混合物定量分析中的多变量色谱校准中的应用

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.008

Erdal Dinç , Abdil Özdemir

{"title":"Linear regression analysis and its application to multivariate chromatographic calibration for the quantitative analysis of two-component mixtures","authors":"Erdal Dinç , Abdil Özdemir","doi":"10.1016/j.farmac.2005.04.008","DOIUrl":"10.1016/j.farmac.2005.04.008","url":null,"abstract":"<div>Multivariate chromatographic calibration technique was developed for the quantitative analysis of binary mixtures enalapril maleate (EA) and hydrochlorothiazide (HCT) in tablets in the presence of losartan potassium (LST). The mathematical algorithm of multivariate chromatographic calibration technique is based on the use of the linear regression equations constructed using relationship between concentration and peak area at the five-wavelength set. The algorithm of this mathematical calibration model having a simple mathematical content was briefly described. This approach is a powerful mathematical tool for an optimum chromatographic multivariate calibration and elimination of fluctuations coming from instrumental and experimental conditions. This multivariate chromatographic calibration contains reduction of multivariate linear regression functions to univariate data set. The validation of model was carried out by analyzing various synthetic binary mixtures and using the standard addition technique. Developed calibration technique was applied to the analysis of the real pharmaceutical tablets containing EA and HCT. The obtained results were compared with those obtained by classical HPLC method. It was observed that the proposed multivariate chromatographic calibration gives better results than classical HPLC.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 591-597"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.04.008","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40936375","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: 19

CV2 - Editorial Board CV2 -编辑委员会

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/S0014-827X(05)00126-6

引用次数: 0

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I 2-氮杂螺[4.4]壬烷和[4.5]癸烷-1,3-二酮的n -苄基和n -氨基苯基衍生物的合成、物理化学和抗惊厥性能。第一部分

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.05.006

Jolanta Obniska , Agnieszka Dzierzawska-Majewska , Agnieszka Zagorska , Pawel Zajdel , Janina Karolak-Wojciechowska

{"title":"Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I","authors":"Jolanta Obniska , Agnieszka Dzierzawska-Majewska , Agnieszka Zagorska , Pawel Zajdel , Janina Karolak-Wojciechowska","doi":"10.1016/j.farmac.2005.05.006","DOIUrl":"10.1016/j.farmac.2005.05.006","url":null,"abstract":"<div>To continue our systematic SAR studies, two series of N-benzyl- (X=CH2) and N-aminophenyl- (X=NH) derivatives of 2-azaspiro[4.4]nonane (1a–1j) and 2-azaspiro[4.5]decane-1,3-dione (2a–2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole (sc.MET) and rotorod (TOX) tests for their anticonvulsant activity. Among those derivatives, the most potent N-aminophenyl-2-azaspiro[4.4]nonane-1,3-dione 1j had ED50 = 76.27 mg kg–1. X-ray structures for two pairs of derivatives with a different linker were solved. Then 3-D data for the active 1j versus less active 2j, both having an imine linker (X  NH), and the respective parent of compounds with a methylene linker (X  <!-->CH2) (1a and 2a) were discussed.</div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 6","pages":"Pages 529-539"},"PeriodicalIF":0.0,"publicationDate":"2005-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.05.006","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25304932","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

Validation of simultaneous volumetric and spectrophotometric methods for the determination of captopril in pharmaceutical formulations 同时体积法和分光光度法测定制剂中卡托普利含量的验证

Farmaco (Societa chimica italiana : 1989) Pub Date : 2005-06-01 DOI: 10.1016/j.farmac.2005.04.005

Nafisur Rahman, Manisha Singh, Md. Nasrul Hoda

引用次数: 21