{"title":"A novel bioactive compounds of 2-azetidinone derived from pyrazin dicarboxylic acid: synthesis and antmicrobial screening","authors":"A. Ayyash, H. Q. A. Habeeb","doi":"10.23893/1307-2080.aps.05727","DOIUrl":"https://doi.org/10.23893/1307-2080.aps.05727","url":null,"abstract":"A series of novel 2-azetidinons entitled N, N’-bis[3-chloro-2-oxo-4-(substituted pyridine-2-yl)-azetidin-1-yl] pyrazine-2,3-dicarboxamide and N,N’-bis[3,3-dichloro-2-oxo-4-(substitutedpyridine-2-yl)-azetidin-1-yl] pyrazine-2,3-dicarboxamide have been synthesized from the relating newly Schiff bases by [2+2] cycloaddition reaction in good yields. Starting with pyrazine-2,3-dicarboxylic acid which was converted to the corresponding diester in absolute ethanol and glacial acetic acid as a catalyst. After that, the hydazinolysis of resulted diester with hydrazine hydrate afforded dicarbohydrazide which further treated with different substituted pyridine-2-carbaldehyde to give new Schiff bases. These new Schiff bases were reacted with chloroacetochloride and (or) dichloroacetochloride in presence of trimethylamine in DMF solvent under reflux and stirring to yield new derivatives of titled compounds. The structural assignments were estimated from their spectroscopic analysis such as IR,1H NMR, 13C NMR, and C, H, N elemental analysis. The newly prepared 2-azetidinones have been screened for their antimicrobial activity and some of them revealed excellent antibacterial and antifungal activities.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68931111","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}
L. Bakre, Damola Osibajo, G. Koiki, Oluyemisi Adebowale Bamiro
{"title":"Material, compressional and tableting properties of ipomea batatas (sweet potato) starch co-processed with silicon dioxide","authors":"L. Bakre, Damola Osibajo, G. Koiki, Oluyemisi Adebowale Bamiro","doi":"10.23893/1307-2080.aps.05722","DOIUrl":"https://doi.org/10.23893/1307-2080.aps.05722","url":null,"abstract":"This study aims to co-process native Ipomea batatas starch (NPS) with colloidal silicon dioxide and evaluate the properties of the co-processed excipient (CPS). The powder morphology was determined by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-Ray Diffraction (XRD) measurements. The compressional, mechanical and release properties of metronidazole tablet formulations were evaluated. NPS was predominantly oval in shape while CPS had more large truncated ellipsoidal granules. Both NPS and CPS exhibited spectra typical of a Type A XRD pattern, but CPS has a sharp peak with strong intensity at 270 2q which was absent in NPS. Although NPS had a faster onset of plastic deformation, the overall amount of plastic deformation was higher in CPS. Tablets formulated with CPS had faster dissolution than those containing similar concentration of NPS. The co-processing of Ipomea batatas starch with colloidal silicon dioxide resulted in modification of its powder and tableting properties.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68931204","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}
Wande M Oluyemi, B. Samuel, Kahlig Hans-peter, Taramelli Donatella, Krenn Liselotte
{"title":"Isolation of two homologous triterpenes with antimalarial activities from the leaf extract of combretum zenkeri","authors":"Wande M Oluyemi, B. Samuel, Kahlig Hans-peter, Taramelli Donatella, Krenn Liselotte","doi":"10.23893/1307-2080.APS.05715","DOIUrl":"https://doi.org/10.23893/1307-2080.APS.05715","url":null,"abstract":"Combretum genus (Combretaceae) is used locally in the treatment of various diseases including malaria. Current study aimed to investigate the antiplasmodial activities of methanol extract of C. zenkeri in Plasmodium falciparum chloroquine sensitive (D10) and resistant (W2) strains and identify the bioactive principles. Repeated chromatographic separation was carried out on the chloroform fraction to afford the isolation of bioactive compounds which was characterized by application of spectroscopic techniques (ESI-MS, HR-ESIMS, 1D and 2D NMR). Antiplasmodial activities of chloroform fraction (D10; IC50= 12.57±1.57 μg/mL and W2; IC50= 12.14±0.95 μg/mL) showed more activity than the n-butanol fraction (D10; IC50= 61.98±3.25 μg/mL and W2; IC50= 61.26±8.64 μg/mL). Phytochemical investigation of the extract afforded isolation of two triterpenes with antimalarial activities. This paper identified for the first time the antimalarial principles in C. zenkeri as ursolic and oleanolic acids; which justified the local use of the plant in the treatment of malaria.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68931349","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":"Dexketoprofen trometamol-loaded eudragit® rl 100 nanoparticle formulation, characterization and release kinetics","authors":"A. A. Öztürk, E. Yenilmez, Y. Yazan","doi":"10.23893/1307-2080.APS.05705","DOIUrl":"https://doi.org/10.23893/1307-2080.APS.05705","url":null,"abstract":"The particle size of the formulations was measured in the range of 475.5-798.7 nm. The droplet size distribution of the formulations was observed in the range of 0.349-0.395. These results showed that nanosized and monodispersed formulations were prepared. The drug content was found to be in the range of 35-38%. DT-loaded particles exhibited nanostructured and spherical shape. In vitro release studies showed extended release of DT. Release was found to fit Korsmeyer-Peppas kinetic model using DDSolver software program.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930136","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":"Estimation of natural radioactivity of some medicinal or herbal plants used in kars, turkey","authors":"G. B. Cengiz, I. Caglar","doi":"10.23893/1307-2080.aps.05729","DOIUrl":"https://doi.org/10.23893/1307-2080.aps.05729","url":null,"abstract":"In Natural radioactive materials may be existing in the environmental substances that have uses in pharmacy and medicine as health supplements. In this study, natural radionuclides such as 226Ra, 232Th, and 40K were measured in seven medicinal or herbal plants collected from the local market in Kars, Turkey were analysed. All samples were analysed by means of gamma-ray spectrometer using NaI(Tl) detector. The radioactivity concentrations were found to vary in the range of 16.39±2.2 to 32.76 ±3.5 Bqkg-1 for 226Ra, 19.74±3.7 to 85.01±5.6 Bqkg-1 for 232Th, and from 795.82±9.8 to 1056.28±14.4 Bqkg-1 for 40K. Rosehip showed the lowest activity concentrations of 226Ra, 232Th and 40K, while rumex patientia showed the highest activity concentration of 40K. In this research study, we aimed to determine the activity concentrations of radionuclides in medicinal plants and provide useful information to carry out a dose assessment to be exposed to people using medicinal plants for healing various diseases.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68931552","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":"A study of drug-excipient interaction and drug product stability using dry (powder) film coating in comparison with conventional (aqueous) film coating","authors":"Derar Omari, Y. Akkam","doi":"10.23893/1307-2080.aps.05719","DOIUrl":"https://doi.org/10.23893/1307-2080.aps.05719","url":null,"abstract":"Solid pharmaceutical dosage forms like tablets, capsules, granules, pellets etc. are coated for many purposes such as protection from moisture, light or oxygen; masking of odor or taste; acid resistance in gastric fluids; and to modify drug release from these dosage forms as controlled or delayed action. Traditionally, coating is carried out using either organic solution or aqueous solution or dispersion of certain polymers sprayed, after mixing with other substances ABSTRACT","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930961","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}
S. R. Devi, Sanjida Jesmin, M. Rahman, M. A. Manchur, Y. Fujii, Y. Ozeki, S. Kawsar
{"title":"Microbial efficacy and two step synthesis of uridine derivatives with spectral characterization","authors":"S. R. Devi, Sanjida Jesmin, M. Rahman, M. A. Manchur, Y. Fujii, Y. Ozeki, S. Kawsar","doi":"10.23893/1307-2080.APS.05704","DOIUrl":"https://doi.org/10.23893/1307-2080.APS.05704","url":null,"abstract":"Uridine is a natural nucleoside precursor of uridine monophosphate in organisms and thus is considered to be safe and is used in a wide range of clinical settings. The farreaching effects of pharmacological uridine have long been neglected. Here, we report a novel series of uridine esters were designed and synthesized by direct method with microbial efficacy. The structures of the prepared compounds have been characterized using various physico-chemical methods including C, H elemental analysis, melting point determination, IR and 1H-NMR spectroscopy. The synthesized uridine derivatives were subjected to in-vitro antibacterial screening using agar disc diffusion method on some clinically isolated Gram-positive and Gram-negative bacterial strains. Also, antifungal functionality test was performed against a number of plant pathogenic fungi. The compounds showed varied antibacterial and antifungal activities. In addition, cytotoxic activity showed different rate mortality with different concentrations. In conclusion, it may useful for antibacterial and antifungal active agents after investigating their further analysis to develop safer and more potent drugs in the future.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930120","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}
B. Giray, L. Yurttaş, Z. Şahin, B. Berk, Ş. Demirayak
{"title":"Antimicrobial evaluation of trisubstituted 2-piperazinyl thiazoles","authors":"B. Giray, L. Yurttaş, Z. Şahin, B. Berk, Ş. Demirayak","doi":"10.23893/1307-2080.APS.05707","DOIUrl":"https://doi.org/10.23893/1307-2080.APS.05707","url":null,"abstract":"Bacterial resistance to the treatment of infectious diseases is the main problem. Many classes of antibiotics are facing resistance and have initiated new efforts to develop new derivatives and discover new chemical classes.1 Gram positive and gram-negative bacteria such as Escherichia coli, Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Bacillus cereus, Pseudomonas aeruginosa etc. are responsible for many diverse infections which even can cause of death.2","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930198","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}
Gülsel Yurtdaş Kırımlıoğlu, E. Yenilmez, E. Başaran, Y. Yazan
{"title":"Preparation and in vitro characterization of a fluconazole loaded chitosan particulate system","authors":"Gülsel Yurtdaş Kırımlıoğlu, E. Yenilmez, E. Başaran, Y. Yazan","doi":"10.23893/1307-2080.aps.05713","DOIUrl":"https://doi.org/10.23893/1307-2080.aps.05713","url":null,"abstract":"In the present study fluconazole (FZ) was successfully incorporated into cationic chitosan nanoparticles prepared by spray-drying method aiming dermal delivery. Particle size and zeta potential measurements, drug content, morphological, thermal and XRD analyses and FZ quantification by HPLC analyses were performed for characterizing the formulations prepared. Release behavior of FZ from the nanoparticles was determined using a Franz-diffusion cell. Thermal and XRD analyses results indicated that FZ was molecularly dispersed in chitosan nanoparticles. Cationic chitosan nanoparticles released FZ for 180 minutes indicative of the extended release of the drug. In vitro characterization results demonstrated that chitosan nanoparticles seem to be promising for enhancement of dermal delivery of FZ and could decrease potential side effects and reduce the potential of drug resistance.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930855","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":"Pharmaceutical properties of marine polyphenols: an overview","authors":"V. Sang, Ngo Dai Hung, Kim Se-kwon","doi":"10.23893/1307-2080.APS.05714","DOIUrl":"https://doi.org/10.23893/1307-2080.APS.05714","url":null,"abstract":"The marine environment represents approximately half of the global biodiversity. It is a rich source of structurally diverse and biologically active metabolites, which are important for the discovery of potential therapeutic agents1, 2. During the last decades, marine organisms have received much attention in screening marine natural products for their biomedical and pharmaceutical potentials3-5. Various marine organisms such as algae, tunicates, sponges, soft ABSTRACT Natural products are non-drug materials that have applied for prevention or treatment of health problem. The use of natural products as pharmaceutical ingredients has got much attention by consumers nowadays. Among them, marine organisms are currently considered as a huge source for the discovery of pharmaceutical agents. During the last decades, numerous novel agents have been achieved from marine organisms and many of them have potential application in pharmaceutical industry. Notably, marine algae are known to be one of the most important producers of variety of chemically active metabolites. Especially, phlorotannins, a polyphenol from brown algae, have been revealed to possess numerous biological activities such as UV-protective, anti-oxidant, anti-viral, anti-allergic, anti-cancer, anti-inflammatory, anti-diabetes, and anti-obesity activities. Therefore, phlorotannins are promising agents for development of pharmaceutical products. This contribution focuses on phlorotannins from brown algae and presents potential application in pharmaceutical field due to its biological activities and health benefit effects.","PeriodicalId":6962,"journal":{"name":"ACTA Pharmaceutica Sciencia","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68930573","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}