bluuebunny/crossref_metadata_2025_split huggingface dataset:
Which activities do great-grandparents and great-grandchildren share in family contexts? An analysis of a new intergenerational relationship.
Authors: Castañeda-García Pedro Javier , Cruz-Santana Vanesa , Hernández-Garrido Fayna , Díaz-Rodríguez Paula , Romero-González Sara 
Published: April 2021

El objetivo general de este trabajo es conocer mejor el rol de bisabuelidad. Se entrevistó a un grupo de voluntarios con bisnietos (n=78) mediante un cuestionario, cuyo contenido fue pilotado previamente, con preguntas sobre sus características sociodemográficas, las actividades que solían compartir con sus bisnietos y su opinión del rol de bisabuelidad, con la satisfacción asociada. Los datos fueron registrados y analizados tanto con tablas de frecuencia y estadísticos descriptivos, como con la prueba no-paramétrica de Kruskal-Wallis. Los resultados obtenidos mostraron numerosas relaciones significativas entre las actividades compartidas y aspectos socio-demográficos de los bisabuelos como la edad (p≤ .05), el nivel educativo (p≤ .01), la salud (p≤ .05), la distancia a la que viven de sus bisnietos (p≤ .05). Además, de mostrar que perciben su rol de bisabuelidad en general como una continuidad del rol anterior de abuelidad, aunque desde una tipología intergeneracional formal, distinta a la tipología informal y, sobre todo, opuesta a la del rol sustituto/subrogado. La mayor satisfacción percibida estaba asociada a esa interacción típica del rol formal (p ≤ .01). Los bisabuelos podrían estar cumpliendo ya alguna función destacable en las familias actuales de cuatro generaciones.
The main aim of this study was to find out more about the role of great-grandparenthood. A group of participants with great-grandchildren (n=78) was interviewed using a questionnaire containing questions that had been put through a previous pilot study, covering participants’ sociodemographics, the activities that participants shared with their great-grandchildren, and their view of the role of great-grandparent and their related degree of satisfaction. The data were recorded and analyzed both with frequency tables and descriptive statistics and with the Kruskal-Wallis non-parametric test. The results showed several significant relationships between the shared activities and the sociodemographic variables, such as great-grandparents’ age (p ≤ .05), education (p ≤ .01), health status (p ≤ .05), the distance at which they live from their great-grandchildren (p ≤ .05). Also, it was found that participants generally consider the role of great-grandparent to be a continuation of their prior role as grandparent, albeit from the perspective of a formal intergenerational typology, distinct from the informal typology and, above all, opposed to the role of substitute/surrogate. Greater perceived satisfaction was associated with this typical interaction of the formal role (p ≤ .01). Great-grandparents may already be fulfilling a notable function in today’s four-generation families.
Duelo complicado: Una revisión sistemática de la prevalencia, diagnóstico, factores de riesgo y de protección en población adulta de España.
Authors: Parro-Jiménez Elena , Morán Noelia , Gesteira Clara , Sanz Jesús , García-Vera María Paz 
Published: April 2021

El objetivo principal de este trabajo fue revisar el estado de la investigación psicopatológica del duelo complicado en población adulta de España. Una búsqueda sistemática en PsycINFO, PsycArticles, PTSDpubs y PSICODOC identificó 13 estudios en los que, en conjunto, se había evaluado a 1,655 adultos. Los resultados de esta revisión ponen de manifiesto que no existe consenso en el diagnóstico de duelo complicado, en el uso de instrumentos de detección ni en los factores de riesgo y protección del duelo complicado. La prevalencia media ponderada basada en 6 de los estudios revisados fue de 21,53%. Tomando en consideración el tipo de instrumento de medida del duelo utilizado, se obtuvo una prevalencia de 7,67-10,68% en aquellos estudios que utilizaban instrumentos diagnósticos y de 28,77% en los instrumentos sintomáticos. Los resultados indican que el duelo complicado se relaciona con: un menor nivel socioeconómico y situación laboral desfavorable, la pérdida de un hijo o cónyuge, menor edad del fallecido, vulnerabilidad psicológica previa, consumo de psicofármacos y comorbilidad con otros trastornos. El apoyo social, los cuidados paliativos, las estrategias de afrontamiento centradas en el problema, el empleo de actividades agradables y la trascendencia o espiritualidad se presentan como factores protectores.

The main objective of this research was to review the status of the psychopathological investigation of complicated grief in adult population of Spain. A systematic review on PsycINFO, PsycArticles, PTSDpubs, and PSICODOC databases identified 13 studies in which, overall, 1.655 adults had been evaluated. The results of this review show that there is no consensus in the diagnosis of complicated grief, in the use of detection instruments, or in the risk and protective factors for complicated grief. The weighted mean prevalence based on 6 of the reviewed studies was 21.53%. Taking into account the type of grief measurement used, a prevalence of 7.67-10.68% was obtained in those studies that used diagnostic instruments and 28.77% in the ones using symptomatic instruments. The results indicate that complicated grief is related to: a lower socioeconomic level and unfavorable work situation, the loss of a child or spouse, younger age of the deceased, previous psychological vulnerability, the use of psychotropic medication and comorbidity with other disorders. Social support, palliative care, problem-centered coping strategies, the use of pleasant activities, and transcendence or spirituality are shown as protective factors.
A New, Cheap, Easy to Use, Foldable and Portable Autocidal Ovitrap for Aedes Control at Community Level
Authors: Carnevale G. , Carnevale P. 
Published: April 2021

Except for Yellow Fever there is still no operational vaccine, the Dengue vaccine (CYD-TDV, sold under the brand name Dengvaxia©) raised several issues and vaccination campaign were stopped. On the other hand there is still no specific treatment for the main arbovirus transmitted by Aedes aegypti and Aedes albopictus such as dengue, Chikungunya, Zika and recent outbreaks occurred all over the World. For WHO “vector control is the key strategy to control or prevent the transmission of dengue (and other arbovirus) but clearly there is a need for improved new vector control approaches. Only another one vaccine is available against arbovirus is against Japanese Encephalitis transmitted by Culex tritaeniorhynchus.
In line with this recommended approaches of new tools to be used at community level we successfully developed and implemented in Angola a “Very Simple Ovitrap Model” which actually “collected” eggs of Aedes aegypti warning for risk of arbovirus outbreaks, which, unfortunately, occurred few years later. These ovitraps were transformed as a tool for vector control in adding few drops of Bacillus thuringiensis (Bt) in the water and several hundred of tests showed that not a single larva of Aedes aegypti was ever found in these “Bt fitted simple ovitrap”.
To solve some operational issues (transport) we tested in Bali during 3 years several size and color of foldable container prepared as ovitraps and put in a garden among grass, banana trees etc, we thus collected eggs of Aedes albopictus, important vector of dengue and dengue hemorrhagic fever (DHF), a serious threat in Asia, and preliminary tests (unpub.) showed some resistance to insecticide increasing the need for control.
According to these trials, made in complete field conditions, we proposed a new foldable model of ovitrap as a vector control tool presented as a kit to be used at community level with a 3 steps action: open it/fill it/use it.
Management of Pediatric both-bone Forearm Fractures by Titanium Elastic Nailing System: A Prospective Study of 60 Cases
Authors: Qureshi Masood Ahmed , Valecha Nuresh Kumar , Keerio Niaz Hussain , Hussain Syed Sajid , Saqlain Hassan Amir us , Jokhio Muhammad Faraz , Noor Syed Shahid 
Published: April 2021

Intramedullary nailing procedure is highly appreciated by many phsyicians for treating pediatrics forearm fractures. Minimum operating time, fewer chances of incisions, faster bone healing, and accuracy in bone alignment less rigid fixation made this technique more popular and preferable. This study was specially designed to observed the management of pediatric both forearm fracture by using the titanium elastic nail technique.
Methodology: Our prospective descriptive study was conducted in King Abdul Aziz Hospital Makkah Saudi Arabia from march 2018 to march 2021. Total 60 patients were enrolled which were treated with titanium elastic nail system (TENS). In this study patients with close displaced and open type 1 fractures with age range of 4 to 14 years were included.
Results: Total 42.5% of participants were under the age of 10, and 57.5% of patients were above 10 years or equal to 10 years age. We reported 58.9% prevelance of injury among male patients. Along with these, we reported 53.4% cases with left side fractures and 60.3% had middle bone fractures. In our study, we reported that the overall average union time was 9.10±1.8.
Conclusion: Titanium elastic nailing is the most effective technique for managing unstable fractures among pediatrics. The male population was more prone to forearm fracture, especially at the middle third shaft. Overall meantime 9 weeks were reported for bone unification. Titanium elastic nailing is more effective technique for patients less than 10 years old. Mean unification time of bone was less among them with little compliactions.
Comparison of the Fluoride Release of Silver Diamine Fluoride, Fluoride Varnish, Acidulated Phosphate Fluoride Gel on Extracted Teeth over Various Time Intervals in Artificial Saliva
Authors: Thakur Taniya , Lahiri Pratik Kumar , Karmakar Madhumanti , Sarvaiya Bhumi , Datta Piyali , Saha Rajib 
Published: April 2021

Silver Diamine Fluoride (SDF) has been documented to effectively arrest dental caries and reduce dental hypersensitivity. SDF promotes remineralization and harden the carious lesion. SDF increases fluoride concentration in saliva and increase the bioavailability of fluoride in saliva. After SDF application, fluoride ion promotes remineralization and silver ion is available for antimicrobial action.
Aim: The study aims to determine and compare the amount of fluoride released from various fluoride releasing materials in artificial saliva after 24 hours, 7th day and 14th day of the study.
Materials and Methods: 96 premolars free of any caries, fractures, or any other defects were sterilized in 10% formalin for 2 weeks. Then they were rinsed in tap water to remove any fixative from its surface and then stored in deionised distilled water for a period of 30 days prior to testing. Tooth samples were divided into four groups- Group 1: 38% SDF, Group 2: 1.23% APF gel, Group 3: Fluoride varnish and Group 4: Control. All the teeth specimens were blot dried and subjected to their respective material. Fluoride release was analysed using a Fluoride ion-selective electrode after 24 hours, 7days and 14 days of suspension in artificial saliva.
Results: Mann-Whitney U Test for inter-group comparison was used for statistical evaluation. 24 Hours fluoride release: The maximum amount of fluoride was released from Fluoride Varnish followed by SDF then APF Gel and least by artificial saliva alone (control) (p<0.001). 7th Day fluoride release: The maximum amount of fluoride was released from SDF followed by Fluoride Varnish then APF Gel and least by artificial saliva alone (control) (p<0.001). 14th Day fluoride release: The maximum amount of fluoride was released from Fluoride Varnish followed by SDF then APF Gel and least by artificial saliva alone (control) (p<0.001).
Provisional BCS Classification of the Leading Oral Drugs on the Global Market
Authors: Dahan Arik , Amidon Gordon L. 
Published: April 2021

Abstract

In the early 1990s, a collaborative research effort between academia and the U.S. Food and Drug Administration (FDA) was initiated to establish a database of human jejunal permeabilities based on a Biopharmaceutics Classification System (BCS). The BCS broadly allowed the prediction of human absorption, Fraction absorbed (
F
abs
) and the rate‐limiting step in the intestinal absorption process of drugs following oral administration. The BCS classified compounds into one of four biopharmaceutical classes according to water solubility and membrane permeability characteristics. Today, the BCS has generated remarkable impact on the global pharmaceutical sciences arena, in drug discovery, development and regulation, and an extensive validation/discussion of the BCS is continuously published in the literature. BCS has been effectively implanted by drug regulatory agencies around the world, and widely practiced by the pharmaceutical industry. The aim of this article is to present the BCS and its scientific basis, to describe its impact on regulatory practice of oral drug products, and to access the BCS classification of the top drugs on the global market. Finally, current and future directions in BCS related extensions, and their impact on the pharmaceutical industry, will be discussed.
Salt Screening and Selection
Authors: Wu Tian , Reid Darren L. , Semin David J. 
Published: April 2021

Abstract

The stability, processability, and
in vivo
performance of active pharmaceutical ingredients (APIs) are significantly affected by their salt forms. The appropriate salt can improve the overall therapeutic and pharmaceutical performance of an API. Salt screening and selection is integrated into the drug discovery and development, and the desired attributes are impacted by multiple factors, including API chemistry, the intended dosage form, pharmacokinetics, and pharmacodynamics. Counterion, solvent, and crystallization are three key elements affecting screening outcomes and selection of the final salt form. Common applications of pharmaceutical salts, general considerations for using salt forms, and a brief acid–base theory related to solubility estimation for salt forms are introduced. A strategy to select counterions and solvents for salt formation is articulated in detail as well as crystallization methodology to harvest highly pure and crystalline salt forms. Three different salt‐screening approaches (
in situ
, rational, and high throughput) are discussed with respect to resource required, project timelines, and the purpose of the study. A four‐tier salt selection strategy is presented, and the desired attributes to meet the target product profile for a typical oral drug are included to guide selection of an appropriate salt from the very initiation of form screen.
Assay Development and High‐Throughput Screening
Authors: Carettoni Daniele , Bader Benjamin 
Published: April 2021

Abstract
High‐throughput screening (HTS) plays a cardinal role in the drug discovery process in pharmaceutical industry and academic institutions. Being the key crossroad between chemistry and biology, it brings into contact the compound library with a functional assay outlining a disease process. Indeed, using a miniaturized functional assay as triaging criterion, HTS ensures a Darwinian selection of a small subset of hit molecules from chemical collections typically exceeding one million compounds. HTS has evolved as an independent multidisciplinary discipline by leveraging several specialties, such as robotics, informatics, molecular biology, recombinant expression technologies, enzymology, cell biology, and combinatorial and medicinal chemistry. Steadily growing technological improvements in HTS have made available an unprecedented array of novel methods and instrumentation that have been contributing to advance the design of functional assays for HTS. Concomitantly, HTS has markedly increased the possibility for low‐throughput/high‐information technologies to be integrated in the drug discovery process at a higher level of processivity. Basically, high‐throughput screening and assay development for HTS are synergistically interconnected, and in this article the multiple points of extensive interdependence are detailed and emphasized. In addition, the sequential steps of the assay development and of the high‐throughput screening are described and examined, describing the state of the art and providing perspective views on the possible future advancements. Most of the concepts of the article are eventually exemplified in a case study on a drug discovery program based on HTS directed against a heterotrimeric protein–protein interaction target.
Anti‐Inflammatory Glucocorticoids
Authors: Avery Mitchell A. , Chittiboyina Amar G. 
Published: April 2021

Abstract

Glucocorticoids are the first line medication used in the treatment of afflictions ranging from the moderate skin rash to severe acute inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand‐dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. The
glucocorticoid receptor
(
GR
) is a cytoplasmic protein of complex structure that is associated with various heat shock proteins (e.g., hsp 90). The desired immunosuppressive effect is apparently due largely to the downregulation of a variety of proinflammatory factors, whereas adverse reactions such as corticoid‐induced diabetes and osteoporosis could be connected to the inappropriate activation of genes involved in the control of metabolic processes. The discovery of selective receptor modulators, which maintain beneficial therapeutic activity together with a diminished risk of side effects, focuses on ligands that lead to repression rather than activation of genes targeted by the glucocorticoid receptor. Current drug‐screening programs have yielded a number of molecules including steroidal as well as nonsteroidal compounds, which preferentially induce receptor‐mediated repression.
Medicinal Chemistry of β‐Lactam Antibiotics
Authors: Testero Sebastian A. , Llarrull Leticia I. , Fisher Jed F. , Mobashery Shahriar 
Published: April 2021

AbstractThe β‐lactam class of antibacterials is a cornerstone of human health. For nearly eight decades, their unparalleled clinical efficacy and clinical safety have made the β‐lactam class preeminent in the treatment of bacterial infection. The relatively brief period in human history during which the β‐lactams have exerted this benefit is a period characterized by continuous medicinal chemistry innovation, seen visibly in the progression from the penicillins to the complex ensemble of β‐lactams (now including also cephalosporins, monobactams, and carbapenems) used in the clinic. The key force behind this innovation is the progressive evolution by bacteria of resistance mechanisms. Today, highly resistant bacteria challenge the way medicinal chemists contemplate the creative alteration of β‐lactam structures, the way the pharmaceutical industry develops β‐lactams (and other antibacterial) structures, and the way the medical community uses antibacterials. This article gives a concise summary of the history of the β‐lactams. Its emphasis is recent structural innovation with respect to the β‐lactams, and with respect to structurally related classes that act to preserve the clinical activity of the β‐lactams through inhibition of bacterial β‐lactam‐hydrolyzing, and thus β‐lactam‐deactivating, enzymes. We integrate these chemistry advances with new biological discoveries with respect to the bactericidal mechanism of the β‐lactams and with respect to bacterial resistance mechanisms. The combination of these perspectives is a foundational perspective to guide the medicinal chemistry future of the β‐lactams.
Translational Pharmaceutics and Early Phase Clinical Development
Authors: Bhattachar Shobha N. , Tan Jeffrey S. , Stamatis Stephen Dion , Hilden Jon 
Published: April 2021

Abstract
Translational pharmaceutics is a relatively new cross‐disciplinary construct that integrates discovery and development for efficiently enabling discovery activities to deliver commercially viable medicines. This article describes the role and deliverables of its various subfunctions, namely, preclinical formulations, physical chemistry, drug product prototyping and development, and biopharmaceutics. The integrated aspects of these deliverables, that enable drug discovery, while also influencing and enabling the selection of compounds for clinical testing, in a manner that embraces the principles of R&D essentialism and design thinking, are also described. This article also illustrates how cost and time savings can be achieved through the application of robust mathematical modeling where possible, to guide the generation of the most relevant experimental data, followed by risk‐based decision‐making to inform commercial product design. Although the article is mostly focused on traditional small molecules, the principles described here can be adapted to include other types of molecular and biologic entities, including the newer molecular modalities that are rapidly gaining importance in the industry.
Artificial Intelligence in Medicinal Chemistry
Authors: Griffen Edward , Dossetter Alexander , Leach Andrew , Montague Shane 
Published: April 2021

AbstractBasic concepts in artificial intelligence (AI) are reviewed with reference to their application in medicinal chemistry. Challenges in the representation of molecules and biological data are discussed. The contrast between AI requiring autonomy and machine learning as a set of statistical techniques is highlighted. Key areas of AI in medicinal chemistry are then reviewed: data extraction, computer aided synthesis planning, compound activity, toxicity and ADME property prediction, automated compound design, and integrating all these tasks into automated drug discovery systems. Finally issues of the adoption of AI methods by medicinal chemists, future developments, and the ethics of AI in medicinal chemistry are addressed.
Sodium Glucose Cotransporter Inhibitors for the Treatment of Diabetes
Authors: Jesus Ana R. , A. Harrison Bryce , Dore Timothy M. 
Published: April 2021

Abstract

Worldwide, the incidence of diabetes mellitus, a chronic metabolic disease that results in four million deaths from it and associated complications annually, is increasing and its treatment is an enormous public health concern. Type 1 diabetes is treated by insulin, but a variety of drugs are used to treat the more prevalent type 2 diabetes. Inhibitors of sodium glucose cotransporters (SGLTs) are the newest drugs to reach the market to achieve the blood‐glucose control needed to treat type 2 diabetes. SGLT1 and 2 carry out renal reabsorption of more than 90% of glucose from urine against a concentration gradient using the electrochemical energy from the cotransport of sodium ions. Blocking SGLTs causes excess glucose to be excreted through the urine, reducing blood sugar. The first known SGLT inhibitor was the
O
‐glycosylated flavonoid natural product phlorizin, which enabled the discovery of SGLTs and served as the initial lead compound for medicinal chemistry.
O
‐ and
C
‐Glycosylated flavonoid and dihydrochalcone natural products also inhibit SGLTs. The drugs on the market today, dapagliflozin, canagliflozin, empagliflozin, ertugliflozin, and others, are all aryl
C
‐glycosides. They are selective for SGLT2 over SGLT1 to avoid adverse side effects associated with SGLT1 inhibition. Studies have suggested that SGLT inhibitors have a renal and cardiovascular protective effect that is advantageous, although their use increases the risk of urinary tract and genital infections and ketoacidosis. SGLT inhibitors are in trials as an adjuvant to insulin for the treatment of type 1 diabetes.