bluuebunny/crossref_metadata_2025_split huggingface dataset:
A Novel Scheme for the Synthesis of 21-Acetoxypregna-1,4,9(11)-triene- 17α,21-diol-3,20-dione from 9α-Hydroxyandrostenedione
Authors: Diep Nguyen T. , Huy Luu D. 
Published: March 2019

Background:
Vietnam currently imports up to 90% of the pharmaceuticals it consumes and
100% of the steroid-based pharmaceuticals. The ability for efficient chemical synthesis of the steroids
could create commercial opportunities to address this issue. Synthesis of 21-acetoxypregna-1,4,9(11)-
triene-17α,21-diol-3,20-dione is considered a key intermediate in the scheme of steroidal drug synthesis.
Previous synthesis attempts of such steroids (corticoids) introduce a double bond at C-1(2) in the final
stage of synthesis, which delivers a poor yield and reduces the economic efficiency of the process.

Objective:
To study and develop a novel and effective method for the synthesis of 21-acetoxypregna-
1,4,9(11)-triene-17α,21-diol-3,20-dione.

Methods:
Using 9α-hydroxyandrostenedione as a substrate chemical synthesis was performed as follows:
pregnane side chain construction at C-17 (acetylene method), introduction of C-1(2) double bond
(using SeO2), epimerization of C-17 (via 17-ONO2 ester) and Stork’s iodination.

Results:
21-acetoxypregna-1,4,9(11)-triene-17α,21-diol-3,20-dione was prepared from 9α-
hydroxyandrostenedione with an improved yield compared to previous attempts.

Conclusion:
Here, 21-acetoxypregna-1,4,9(11)-triene-17α,21-diol-3,20-dione has been synthesized
from 9α-hydroxyandrostenedione based on a novel, effective and commercially feasible scheme. The
introduction of the C-1(2) double bond at an earlier stage of the synthesis has increased the economic
efficiency of the entire process. For the first time, the indirect epimerization mechanism has been clarified
along with the configuration of the C-17 stereo-center which has been confirmed using NOESY
data.
Docking, Synthesis and Antimalarial Evaluation of Hybrid Phenyl Thiazole 1,3,5-Triazine Derivatives
Authors: Das Arpita , Ghosh Surajit K. , Bhat Hans Raj , Kalita Junmoni , Kashyap Ankita , Adhikari Nayana 
Published: March 2019

Background:
Presentlytheeffectiveness of antifolate antimalarial drugs is decreasing due to
the emergence of resistant Plasmodium strains. The aim of the present study was to determine the antimalarial
effect of hybrid p-bromo phenyl thiazole-triazine derivatives against 3D7 strain of Plasmodium
falciparum.

Methods:
Seventy-fivehybrid derivativeswere designed based on the lead molecule and docking was
done against the active site of Pf-DHFR-TS (PDB i.d. 1J3i) with validated ligand fit protocol by using
Discovery Studio 2.5. Based on the highest binding energy and the best docked pose, fifteen compounds
were selected for the synthesis. Synthesized compounds were characterized by different spectroscopy
methods and in-vitro antimalarial evaluation was done against the 3D7 strain of Plasmodium falciparum.

Results:
Fifteen compounds were synthesized by conventional and microwave assisted method and
were characterized byFT-IR, 1H-NMR, 13C-NMR and Mass spectroscopy. In-vitro antimalarial screening
results showed that compounds ADG303, ADG 306 and ADG 302 have the highest activity against
3D7 strain of P. falciparum. Furthermore, docking result of these compounds having binding energies
of -154.91, -165.981, -137.826 respectively showed similarity with reference compound WR99210
(-152.023) and also bound to Asp54 and Phe 58 amino acid at the active site of the receptor.

Conclusion:
The synthesized compound ADG303 exhibited an encouraging result which could be a
new lead for antimalarial drug discovery.
Assessment of Hepatoprotective and Antiulcer Activity of Launaea aspleniifolia Hook in Laboratory Animals
Authors: Ali Sadik , AnupMaiti  , Vishwakarma Vishal Kumar , Ajay Kumar 
Published: March 2019

Background:
Launaea aspleniifolia Hook (Family Asteraceae) is used traditionally in medicine
in Indian system for the treatment of leucoderma. This study was conducted to evaluate the hepatoprotective
and antiulcer effects using the methanolic extract of Launaea aspleniifolia Hook (MELA).

Methods:
The MELA in the dose of 200 and 400 mg/kg body weight (b.w.) was administered orally,
daily for 7 days to prevent the acetaminophen-induced hepatotoxicity and peptic ulcer. In order to determine
the antioxidant enzymes activity, various enzymatic parameters including alanine aminotransferase
(ALT), aspartate aminotransferase (AST), total bilirubin (TBL), direct bilirubin (DBL), alkaline
phosphatase (ALP), total protein (TP), albumin (ALB), high density lipoproteins (HDL), random glucose
test (RBS), serum creatinine levels (SCL) and direct bilirubin (DBL) were determined. Further, the
histopathology of tissue and various gastric secretion parameters like free acidity, total acidity ulcer
score, % ulcer inhibition, gastric volume, pH, Na+ and K+ and histopathology were determined in PLinduced
ulcer model.

Results:
MELA showed dose-dependent hepatoprotective and ulcer protective effect in acetaminopheninduced
hepatotoxicity and antiulcer activity. Furthermore, tissue antioxidant parameter such as reduced
Malondialdehyde (MDA), histopathology was also investigated. MELA was more potent in controlling
all the serological parameter of liver like ALT, AST, TBL, DBL, ALP, HDL, RBS, SCL, TP and ALB
in a dose-dependent manner (P<0.05) induced by Acetaminophen. Apart from this, antiulcer activity
MELA was confirmed by the low level of ulcer index along with the reduction of free acidity, total acidity
ulcer score, % ulcer inhibition, gastric volume, Na+ and an increase K+, pH of gastric content in a
dose-dependent manner (P<0.05) induced PL model.

Conclusion:
The results indicated a significant dose-dependent effect of MELA from injuries induced
in liver and stomach. These protective effects of MELA can be examined in various other toxicities as
alone and in combinations.
Bioactivity Guided Fractionation and Purification of Anti-Depressant Molecule from Ashwagandha (Withania somnifera)
Authors: Antony Benny , Aravind A.P.A. , Benny Merina , Gupta Nishant K. , Joseph Biji , Sebastian Anu 
Published: March 2019

Background:
Ashwagandha (Withania somnifera) is an important herb in the Indian traditional
system of medicine for neurological disorders. However, the efforts for isolation and
characterisation of a molecule with anti-depressant activity and development as a potent dosage form
are limited.

Objective:
The objective of the present study was to characterize the Ashwagandha extract for its antidepressant
fraction or constituent and to improve biological benefits at low doses.

Methods:
Aqueous methanol extract of Ashwagandha was prepared and fractionated into withanolides
and flavonoids rich fractions. Withanolide rich fraction was subjected to phytochemical analysis to identify
the active molecule/s. The compound was purified by using a semi-preparative HPLC system; identified
using various spectroscopic techniques and anti-depressant activity was evaluated in rats. Enteric
coating was performed on the extract and fractions after granulation and anti-depressant activity of
coated samples were evaluated in rats.

Results:
Aqueous methanol extract of Ashwagandha and withanolide rich fraction showed prominent
dose-dependent anti-depressant activity in forced swim test in rats. Phytochemical analysis of active
fraction resulted in the isolation and characterization of a major withanolide glycoside present, namely
withanoside X. Enteric coated aqueous methanol extract, withanolide rich fraction and withanoside X
showed significant antidepressant activity at low doses as compared to the uncoated forms.

Conclusion:
The active fraction/isolated compound is sensitive to low pH of the stomach, thus enteric
coating might be beneficial to protect the actives in the stomach, facilitating the sustainable release into
the intestine and in turn reduce the dosage.
Ramelteon in the Treatment of Delirium: New Perspectives from Reported Findings and a Case Observation
Authors: Sanchez Deborah L. , Fusick Adam J. , Hudson William B. , Schmitz Jourdan E. , Catalano Maria C. , Catalano Glenn 
Published: March 2019

:Ramelteon is a melatonin receptor agonist that is approved for the treatment of insomnia. It is widely used due to its relatively benign side effect profile and lack of dependence or withdrawal. Due to its tolerability, clinicians have attempted to utilize ramelteon to normalize the sleep/wake patterns in patients with delirium as a safer alternative to antipsychotics or other medications. We present the case of a 75-year-old man with long-standing dementia who was hospitalized due to mental status changes, agitation, and sleep disturbance. After addressing possible underlying causes with minimal improvement, the team initiated treatment with ramelteon (8mg nightly) which resulted in rapid improvement of symptoms. Uses and mechanisms of action of ramelteon will be reviewed, as well as current pharmacologic treatments of delirium. Prior research studies and case reports regarding the use of ramelteon in the treatment of delirium will be discussed and suggestions made regarding possible areas of future study.
Evaluation of Pyrano[3,2 C] Quinoline Analogues as Anticancer Agents
Authors: Upadhyay Kuldip D. , Shah Anamik K. 
Published: March 2019

Background:Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents.Objective:The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from the fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity.Methods:A library of pyrano[3,2-c]quinoline analogues was prepared from one-pot multi component synthesis using various aromatic aldehydes, malononitrile and 2,4-dihydroxy-1-methylquinoline. The new synthetics were primarily screened for its cytotoxicity (IC50) against different human cancer cell lines in vitro. The promising synthetics were further evaluated in vitro for their potency against different kinase activity. The promising compounds were finally tested for their in vivo efficacy in SCID type mice HCT-116 tumor model.Results:The screening results revealed that compounds 4c, 4f, 4i and 4j showed promising activity in in vitro study. However, compound 4c was found to be the most potent candidate with 23% tumor growth inhibition in HCT-116 tumor mice model.Conclusion:The structure activity relationship suggested that 3-substitution on the aryl ring at C4 position of the pyrano[3,2 c]quinolone moiety seems to have an important position for cytotoxicity activity. However, 3- chloro substitution at C4 aryl ring showed a significant alteration of the bioactive conformer of the parent scaffold and outcome with compound 4c as the most potent candidate of the series.
The Value of Soluble Transferrin Receptor and Soluble Transferrin Receptor-ferritin Index in Discriminating Iron Deficiency Anaemia from Anaemia of Chronic Disease in Patients With Rheumatoid Arthritis
Authors: Al-Rubaie Haithem A. , Al-Bayaa Israa M. , Al-Amiri Yassmin A. 
Published: March 2019

Background:Anaemia is a common extra-articular manifestation of rheumatoid arthritis (RA) where anaemia of chronic disease (ACD) and iron deficiency anaemia (IDA) are the two most frequent types. The distinction between these two types of anaemia has always been challenging requiring sophisticated techniques. Serum transferrin receptor (sTfR) a truncated soluble form of the transferrin receptor is one of the parameters that is influenced by the Iron content and supply to the erythrons and is not affected by inflammatory status and therefore the use of the sTfR/log ferritin (sTfR-F) index can be a reliable indicator of functional iron deficiency.Aim of the study:This study aims to evaluate the usefulness of sTfR and sTfR-F index in discriminating the most common types of anaemia in patients with RA.Patients and methods:The study included 50 patients with RA and 30 healthy subjects as a control group. Complete blood picture, C-reactive protein, serum Iron, unsaturated iron binding capacity, sTfR and serum ferritin were tested.Results and Conclusion:anaemia was present in 34/50 patients; 19 patients had ACD, 9 had ACD/IDA and only 6 patients had IDA. Both the sTfR and the sTfR-F index showed a significant difference between anaemia groups (P values = 0.037 and 0.001, respectively). sTfR-F index has shown to be a very useful parameter that can discriminate efficiently between IDA and ACD and between ACD and ACD/IDA in patients with RA.
Investigation of Optical and Dielectric Constants of Benzobis(thiazole)- based Copolymer Films
Authors: Su Yue , Yang Ailing , Zhang Wenzhe , Wen Shuguang 
Published: March 2019

Introduction:
Copolymer PBB-T with benzo[1,2-d:4,5-d']bis(thiazole) (BBT) as the
accepting unit and benzodithiophene (BDT) as the donor unit is a promising candidate for highperformance
non-fullerene polymer solar cells (PSCs). So far optical and dielectric constants of the
PBB-T are not fully known.

Method:
PBB-T was synthesized and thin films of PBB-T were prepared. By using the Kramers-Kronig
relations and the transmission spectra of the PBB-T films, the optical and dielectric constants, including
in absorption coefficient (α(λ)), extinction coefficient (κ(λ)), refractive index (n(λ)), dielectric constant
(ε1(λ),ε2(λ)), band gap (Eg) and mobility of the PBB-T films were calculated and analyzed.

Result:
At 500 nm, α, κ, n, ε1 and ε2 are 1.65×105 cm-1, 0.46, 1.8163, 3.0 and 1.65 respectively.
Eg is 2.111 eV. The hole mobility of PBB-T are 2.41×10-5 cm2 V-1 s-1 and 1.71×10-4 cm2 V-1 s-1 for
the as-cast film and for the solvent vapor annealed film respectively. The results show that these
optical and dielectric constants of the PBB-T films are almost independent on the thicknesses of
the films, indicating our results are reliable. The features of the optical and dielectric constants
show the PBB-T films are very promising candidates for high-performance non-fullerene PSCs
and potential cut-off filter only permitting red and near-infrared light passing.

Conclusion:
These results are significant for designing optoelectronic devices related to the PBBT
thin films.
Unusual Enthalpy Driven Self Assembly at Room Temperature with Chitosan Amphiphiles
Authors: Odunze Uchechukwu , O'Brien Fionn , Godfrey Lisa , Schätzlein Andreas , Uchegbu Ijeoma 
Published: March 2019

Background:
GCPQ (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-
6-O-glycolchitosan) is a self-assembling polymer being investigated as a pharmaceutical
nano-carrier. GCPQ nanoparticles shuttle drugs across biological barriers, improving
drug performance. The exact chemistry of GCPQ is varied by the relative proportion of
hydrophobic (N-palmitoyl) and hydrophilic (quaternary ammonium) groups and molecular
weight.

Objective:
We hypothesised that the thermodynamics of self-assembly is controlled by the
polymer molecular weight and hydrophobicity.

Method:
The thermodynamics of self-assembly was investigated using isothermal calorimetry.

Results:
GCPQs (Mw = 8-15 kDa) formed micellar aggregates at critical micellar concentrations
of 1-2.4 µM at 25°C and micellisation was unusually enthalpy driven. There was a
positive correlation between ΔHmic and mole% quaternary groups (Q): ΔHmic = 3.8 Q-
159 (r2 = 0.93) and a negative correlation between ΔHmic and molecular weight (Mw):
ΔHmic = -13.5 Mw-26.3 (r2 = 0.99).

Conclusion:
These findings provide insights into the positive drivers of stable selfassemblies,
namely hydrophobicity and molecular weight, as both hydrophobicity and molecular
weight are associated with an increased enthalpy contribution to micellisation.
Understanding the Significance of Microwave Radiation for the Graft Copolymerization of Acrylamide on Carboxymethyl Xanthan Gum
Authors: Badwaik Hemant R. , Alexander Amit , Sakure Kalyani 
Published: March 2019

Background:
Nowadays, microwave assisted techniques are becoming popular ecofriendly
approaches in Green Chemistry. However, to date, no study has reported the microwave assisted
graft copolymerization of acrylamide on carboxymethyl xanthan gum backbone.

Objective:
The objective of this study was to study the effect of microwave radiations on graft copolymerization
of acrylamide on carboxymethyl xanthan gum.

Methods:
Carboxymethyl xanthan gum was grafted with acrylamide under microwave irradiation.
The grafting process is optimized by varying the amount of carboxymethyl xanthan gum, acrylamide,
ammonium persulphate, microwave power and exposure time. The graft copolymer was further characterized
and evaluated for its efficacy.

Results:
Grafting was successfully optimized for higher grafting efficiency (92.4 %) and grafting
(410.5 %) in a short reaction time of 150 s, at 40 times less concentration of ammonium persulphate.
The characterization study confirmed the grafting of acrylamide on the hydroxyl group of carboxymethyl
xanthan gum backbone.

Conclusion:
Microwave radiations play a vital role in graft copolymerization of acrylamide on carboxymethyl
xanthan gum, in short reaction time, at 40 times less concentration of initiator. The synthesized
graft copolymers remain nontoxic and also showed more antimicrobial activity than carboxymethyl
xanthan gum.
Organophotoredox Catalysis: Visible-light-induced Multicomponent Synthesis of Chromeno[4, 3-b]chromene and Hexahydro-1H-xanthene Derivatives
Authors: Sharma Amit K. , Tiwari Jyoti , Jaiswal Deepali , Singh Shailesh , Singh Jaya , Singh Jagdamba 
Published: March 2019

Background:In recent years, photoredox catalysis using eosin Y has gained considerable significance in organic chemistry. It is evolving as a powerful approach in modern organic synthesis for the activation of small molecules.Objective:The use of organic dyes to convert visible light into chemical energy by involving a single-electron transfer with organic substrates has innumerable applications.Method and Results:The present strategy is the first example of visible light promoted, aerobic, oxidative cyclization of chromeno[4,3-b]chromenes and hexahydro-1H-xanthenes via the formation of C–O and C–C bonds to afford excellent yield of the products in a simple one-pot operation under mild reaction conditions.Conclusion:The major advantages of the present methodology include short reaction time, cost effectiveness, easy work-up, broad substrate scope and high atom economy.
Economic burden and treatment patterns for patients with diffuse large B-cell lymphoma and follicular lymphoma in the USA
Authors: Ren Jinma , Asche Carl V , Shou Yaping , Galaznik Aaron 
Published: March 2019

Aim:
Diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL) are common types of non-Hodgkin's lymphoma, and real-world evidence continues to be lacking for healthcare costs and utilization among DLBCL and FL patients. Our study aims to describe medical and pharmacy costs and health resource utilization and to characterize longitudinal treatment patterns among these patients.
Methods:
A retrospective observational study was performed among adult patients with DLBCL or FL using the US MarketScan (Truven) administrative claims data from 1 January 2007 to 31 December 2015. Diagnoses of DLBCL and FL were based upon ICD-9 codes. Identifications of treatment lines involved 30 lymphoma-specific anticancer systemic agents. Direct healthcare costs and utilizations were computed in the 1-year postdiagnosis period. Generalized linear models with a gamma link were used to compare healthcare costs between therapies with and without rituximab.
Results:
A total of 2767 DLBCL and 5989 FL patients received frontline therapy. The majority received treatment within 3 months after initial diagnosis (DLBCL 79.9% and FL 62.4%) and were treated with rituximab or bendamustine either alone or in combination (DLBCL 67.4% and FL 84.7%). The total healthcare costs were US $15,555 and $10,192 per patient per month within 1 year following their initial diagnosis for DLBCL and FL, respectively. The medical costs were nearly twice as much as the drug costs for DLBCL patients. Both DLBCL and FL patients receiving rituximab had higher pharmacy costs but lower medical costs (p < 0.001). During the first year following initial diagnosis, the resource utilization (per patient per month) of DLBCL patients included 0.21 inpatient admissions, 0.26 radiation therapy, 2.63 outpatient or office visits, 0.18 emergency room visits, 0.06 intensive care unit admissions and 0.10 stem cell transplantation. FL patients occupied less health resources than DLBCL patients.
Conclusion:
The healthcare costs and health resources utilized were considerable in non-Hodgkin's lymphoma, especially DLBCL patients.
Relación entre estrategias de aprendizaje y rendimiento académico: estudiantes de enfermería, Universidad Santo Tomás
Authors: Mercado-Elgueta C. , Illesca-Pretty M. , Hernández- Díaz A. 
Published: March 2019

Las estrategias de aprendizaje son actividades o procesos mentales que llevan a cabo los/as estudiantes, intencionalmente para procesar, entender y adoptar la información que reciben en el proceso educativo.
Objetivo: Describir las estrategias de aprendizaje de estudiantes de la Carrera de Enfermería, Universidad Santo Tomás Temuco-Chile, y determinar la correspondencia entre ellas con el rendimiento académico y variables sociodemográficas.
Métodos: Se realizó un estudio no experimental de corte transversal. La muestra, no-probabilística, de conveniencia, conformada por 185 estudiantes de enfermería de todos los niveles. Se utilizó la Escala de Estrategias de Aprendizaje ACRA-Abreviada (Adquisición, Codificación, Recuperación y Apoyo de la información). Se usó el Programa Stata 11.0, para comparar promedios la prueba t-test y ANOVA, y la correlación de Pearson, para la relación entre variables cuantitativas.
Resultados: Los estudiantes emplean un número importante de estrategias, principalmente las de repetición y relectura (adquisición) y las de apoyo social (apoyo). Las mujeres utilizan más estrategias que los hombres, encontrándose diferencias en las de selección y organización (codificación) de elaboración (codificación) y de subrayado (adquisición). No se encontraron relaciones consistentes entre el uso de estrategias y el rendimiento académico.
Conclusión: Se conocen un número importante de estrategias y hacen uso de ellas, pero no de manera profunda, empleándolas básicamente como elementos de memorización y apoyo al aprendizaje. Se propone, realizar diagnóstico de estrategias al ingreso universitario, capacitación docente y establecer programas donde se promueva la capacidad en los educandos de gestionar su aprendizaje, y la evaluación autentica de los contenidos.