Abstract:
:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned structures were verified by IR, 1H-NMR, and mass spectral studies. Six compounds of the series were screened for in vitro antibacterial and antifungal activities. The effect of four compounds on alkaline phosphatase enzyme was also examined.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Soliman FS,Shafik RM,Darwish Mdoi
10.1002/jps.2600710210subject
Has Abstractpub_date
1982-02-01 00:00:00pages
178-82issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)44036-5journal_volume
71pub_type
杂志文章abstract::Formulation pH has been reported to be responsible for the incidence of phlebitis. In this study, the effect of pH on injection phlebitis is investigated. Buffers of varying pHs were examined for their ability to produce phlebitis in rabbits. Thermal measurements as well as visual evaluations were used for phlebitis q...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600840427
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abstract::The positively charged amino acids are commonly used excipients in biopharmaceutical formulations for stabilization of therapeutic proteins, yet the mechanisms for their modulation of protein stability are poorly understood. In this study, both lysine and histidine are shown to affect the thermal stability of myoglobi...
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journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600670247
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abstract::The present study aimed to develop optimized quercetin (QT)-loaded self-nanoemulsifying drug delivery system (SNEDDS) that offers protective effect against liver damage. Solubility study of QT in different oils, surfactants, and cosurfactants was performed. Ternary phase mixtures of the selected components were constr...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.23834
更新日期:2014-02-01 00:00:00
abstract::beta-Cyclodextrin was ethylated at the 2- and 6-hydroxyl positions. Diethyl sulfate was employed as an alkylating reagent. NMR spectra data indicate that heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (DCD) is the principal component of the product obtained. In addition, the FAB mass spectra obtained in nitrobenzyl alcoho...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840819
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abstract::A GLC method is described for the determination of iminodibenzyl and desipramine impurities in imipramine hydrochloride and its formulated products. These impurities were extracted from an alkaline solution with a mixture of 30% methylene chloride in hexane for chromatography on a 3% OV-17 GLC column. Iminodibenzyl wa...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600710515
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abstract::A high-performance liquid chromatographic method with spectrofluorometric detection has been developed for the analysis of a new substituted benzamide and its metabolite in body fluids. The detection was performed at 270 nm for excitation, and 370 nm for emission. The proposed technique is selective, reliable, and sen...
journal_title:Journal of pharmaceutical sciences
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abstract::A new method for determining a quaternary mixture of vitamins B6, B1, and B12 and uridine 5'-triphosphate (UPT) using second-derivative spectrophotometry is described. Calibration graphs were linear up to 30 micrograms/mL of vitamin B6 at 307 nm (r = 0.9999) and vitamin B1 at 282.7 nm (r = 0.9997) and up to 35 microgr...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600840109
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abstract::Chloroquine (7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline; CQ) accumulates in the insoluble fraction of rat muscle homogenates with an equilibrium distribution ratio of 7.8 L/kg. This is of a similar magnitude to muscle:plasma ratios observed in vivo. Uptake is approximately linear, even up to concentra...
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journal_title:Journal of pharmaceutical sciences
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更新日期:1984-12-01 00:00:00
abstract::A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600641213
更新日期:1975-12-01 00:00:00
abstract::Electron micrographs of Pseudomonas aeruginosa grown in nutrient broth or broth containing subinhibitory concentrations of benzalkonium chloride indicate that benzalkonium chloride at 50 and 100 mug/ml strips off the outer cell membrane. Cells grown in the presence of edetate disodium, 50-100 mug/ml had convoluted sur...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600650115
更新日期:1976-01-01 00:00:00
abstract::An HPLC methodology is described which enables the quantitation of thiothixene (N,N-dimethyl-9-[3-(4-methyl-1-piperazinyl)-propylidene]thioxanthe ne-2- sulfonamide) in bulk drug, finished product, and dissolution samples using a single analytical column (SiAl: a mixture of silica and alumina). The Z (cis) and the less...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600760310
更新日期:1987-03-01 00:00:00
abstract::The granule strength (crushing load) of lactose granulated with 1-9% povidone was measured initially and at intervals during a 1-year period. The granule strengths of dibasic calcium phosphate dihydrate granulated with various concentrations of starch and povidone were measured. The axial and radial tensile strengths ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600720513
更新日期:1983-05-01 00:00:00
abstract::A physiologic pharmacokinetic model describing percutaneous absorption of topically applied compounds in the isolated perfused porcine skin flap (IPPSF) is presented. As an extension of a previously reported hybrid physiologically relevant compartmental model of uptake of intra-arterially administered drug in the IPPS...
journal_title:Journal of pharmaceutical sciences
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doi:10.1002/jps.2600790407
更新日期:1990-04-01 00:00:00
abstract::The health effects of green tea are associated with catechins: (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin, (-)-epicatechin-3-O-gallate, and (-)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biol...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.07.026
更新日期:2018-11-01 00:00:00
abstract::The α-keto carboxylic acid, pyruvic acid (1) was found to be a very effective peroxide scavenger but is subject to an aldol-like self-condensation/polymerization reaction. The purpose of this study was to evaluate the hydrogen peroxide, H2O2, scavenging ability of 3-methyl-2-oxobutanoic acid (2), 4-methyl-2-oxopentano...
journal_title:Journal of pharmaceutical sciences
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doi:10.1016/j.xphs.2016.03.041
更新日期:2016-09-01 00:00:00
abstract::A theoretical investigation has been conducted to understand the deconvolution method used for evaluating the in vivo release rate of an oral controlled-release product from the plasma drug concentration versus time profile. The theory is based on well-accepted pharmacokinetic compartmental models. The cumulative amou...
journal_title:Journal of pharmaceutical sciences
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更新日期:1993-11-01 00:00:00
abstract::A number of biopharmaceuticals are available as lyophilized formulations along with a prefilled syringe (PFS) containing water for injection (WFI). Submicron- and micron-size droplets of lubricating silicone oil (SO) applied to the inner surface of the PFS barrel might migrate into the WFI, to which protein pharmaceut...
journal_title:Journal of pharmaceutical sciences
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abstract::Near infrared (NIR) spectroscopy was used for quantitatively monitoring polymorph conversion of an active pharmaceutical ingredient (API) in wet granulation. The API under pharmaceutical development has two different polymorphs. Polymorph A is the stable form for drug development and polymorph B is the undesired form ...
journal_title:Journal of pharmaceutical sciences
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更新日期:2005-12-01 00:00:00
abstract::Each of three harmala alkaloids, harmine, harmaline, and harmalol, decreased heart rate and increased pulse pressure, peak aortic flow, and myocardial contractile force in intact normotensive anesthetized dogs. Harmine reduced systemic arterial blood pressure and total peripheral vascular resistance; harmaline-evoked ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600660910
更新日期:1977-09-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830629
更新日期:1994-06-01 00:00:00
abstract::The purpose of this study was to elucidate the effect of heat treatment on the miscibility of multiple concentrated solutes that mimic biopharmaceutical formulations in frozen solutions. The first heating thermal analysis of frozen solutions containing either a low-molecular-weight saccharide (e.g., sucrose, trehalose...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22706
更新日期:2011-12-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21673
更新日期:2009-11-01 00:00:00
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journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600691218
更新日期:1980-12-01 00:00:00
abstract::Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...
journal_title:Journal of pharmaceutical sciences
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journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20980
更新日期:2007-12-01 00:00:00
abstract::An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600760716
更新日期:1987-07-01 00:00:00
abstract::An in vitro technique was developed to characterize the intermittent flume patterns associated with the short bursts of metered-dose aerosols. Two orthogonal video images are utilized to describe the complex shape and direction of the flume pattern. This technique facilitates the evaluation of components manufactured ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600690628
更新日期:1980-06-01 00:00:00