bluuebunny/crossref_metadata_2025_split huggingface dataset:
Trimethoxy Crown Chalcones as Multifunctional Class of Monoamine
Oxidase Enzyme Inhibitors
Authors: Maliyakkal Naseer , Ucar Gulberk , Mathew Bijo , Baysal Ipek , Tengli Anandkumar , Almoyad Mohammad Ali Abdullah , Parambi Della Grace Thomas , Gambacorta Nicola , Nicolotti Orazio , Beeran Asmy Appadath 
Published: June 2021

Background:
Chalcones with methoxy substituent are considered as a promising
framework for the inhibition of monoamine oxidase (MAO) enzymes.

Methods:
A series of nine trimethoxy substituted chalcones (TMa-TMi) was synthesized and
evaluated as a multifunctional class of MAO inhibitors. All the synthesized compounds were
investigated for their in vitro MAO inhibition, kinetics, reversibility, blood-brain barrier (BBB)
permeation, and cytotoxicity and antioxidant potentials.

Results:
In the present study, compound (2E)-3-(4-nitrophenyl)-1-(3,4,5-trimethoxyphenyl)prop-
2-en-1-one (TMf) was provided with a MAO-A inhibition constant value equal to 3.47±0.09 μM
with a selectivity of 0.008, thus comparable to that of moclobemide, a well known potent hMAOA
inhibitor (SI=0.010). Compound (2E)-3-(4-bromophenyl)-1-(3,4,5-trimethoxyphenyl)prop-2-
en-1-one (TMh) show good MAO-B inhibition with inhibition constant of 0.46±0.009 μM. The
PAMPA assay demonstrated that all the synthesized derivatives can cross the BBB successfully.
The cytotoxicity studies revealed that TMf and TMh have 88.22 and 80.18 % cell viability at 25
μM. Compound TMf appeared as the most promising antioxidant molecule with IC50 values,
relative to DPPH and H2O2 radical activities equal to 6.02±0.17 and 7.25±0.07 μM. To shed light
on the molecular interactions of TMf and TMh towards MAO-A and MAO-B, molecular docking
simulations and MM/GBSA calculations have been carried out.

Conclusion:
The lead molecules TMf and TMh with multi-functional nature can be further
employed for the treatment of various neurodegenerative disorders and depressive states.
Association of Variants in FCGR2A, PTPN2, and GM-CSF with Cerebral Cavernous Malformation: Potential Biomarkers for a Symptomatic Disease
Authors: da Fontoura Galváo Gustavo , Fontes-Dantas Fabrícia Lima , da Silva Elielson Veloso , Alves-Leon Soniza Vieira , de Souza Jorge Marcondes 
Published: June 2021

Backgrounds:
Cerebral Cavernous Malformations (CCM) predispose patients to a lifetime
risk of seizures and symptomatic hemorrhage. Only a small percentage of people affected will
develop clinical symptoms and the molecular mechanisms underlying lesional activity remain unclear.
We analyzed a panel of Single Nucleotide Polymorphisms (SNPs) in CCM patients. We
looked for plasmatic inflammatory cytokines, checking for a pattern of plasma expression heterogeneity
and any correlation with genetic variations identified with different CCM clinical phenotypes.

Methods:
This was a case-control study from a long-term follow-up cohort including 23 CCM patients,
of which 16 were symptomatic, and 7 were asymptomatic. A 200-SNP panel was considered
through next-generation sequencing and 18 different plasma molecules were assessed through a suspension
array system.

Results:
Fcγ receptor IIa rs1801274 (FCGR2A) and protein tyrosine phosphatase non-receptor type
2 rs72872125 PTPN2 were statistically different between groups. Patients who had a combination
of the presence of FCGR2A and the absence of PTPN2 also had symptoms earlier in life. The combination
of genetic polymorphisms and serum level of GM-CSF showed the best diagnostic biomarker
to distinguish symptomatic patients as formulated: [0.296*(FCGR2A)] + [-0.788*(PTPN2)]
+ [-0.107*(GM-CSF)].

Conclusion:
We have shown that SNPs in inflammation genes might be related to a symptomatic
phenotype in CCM. We also demonstrated that a formula based on two of these polymorphisms
(FCGR2A+ and PTPN2+) is possibly capable of predicting a symptomatic phenotype during a patient’s
lifetime.
Synthesis of Substituted -N-(5-((7-Methyl-2-Oxo-2H-Chromen-4-yl)-
Methyl)-1,3,4-Thiadiazol-2-yl)-Benzamide Derivatives Using TBTU as
Coupling Agent and their Evaluation for Anti Tubercular Activity
Authors: Kakadiya Monika , Pasha Yunus , Noolvi Malleshappa , Patel Ashish 
Published: June 2021

Abstract:
Tuberculosis remains a highly infectious disease across the world. In the identification of
new antitubercular agents, coumarin clubbed thiadiazole amides have been synthesized and evaluated
for in vitro antitubercular activity. Owing to the growing concern of chemicals and their impact on the
environment, greener and faster reaction conditions needed to be incorporated. Therefore, we used
TBTU as a coupling reagent for efficient and facile synthesis of substituted-N-(5-((7-methyl-2-oxo-2Hchromes-
4-yl)-methyl)-1,3, 4-thiadiazol-2-yl)-benzamide 4a-j with good yields up to 95% in mild reaction
conditions. All the synthesized compounds were evaluated in vitro for anti-tubercular activity
against the H37Rv strain of M. tuberculosis. Compounds 4c, 4d, and 4f were found active at 12.5
μg/mL against M. tb H37Rv. Electron withdrawing substituents present on aromatic side chains showed
promising anti-tubercular activity.
3D-QSAR, Docking, and Molecular Dynamics Simulations Studies on Quinazoline Derivatives as PAK4 Inhibitors
Authors: Chen Xiao-Zhong , Dai Chen , Shen Yan , Wang Juan , Hu Yong , Wang Yuan-Qiang , Lin Zhi-Hua 
Published: June 2021

Background:
The p21-activated kinases 4 (PAK4) refer to a promising target for cancer
treatment. Currently, a wide range of PAK4 inhibitors has been reported.

Objective:
The objective of this study is to study the structural requirements of quinoline derivatives
as PAK4 inhibitors and to design novel PAK4 inhibitors.

Methods:
In the present study, a set of quinazoline PAK4 inhibitors underwent CoMFA, CoMSIA,
molecular docking, as well as molecular dynamics simulations.

Results:
The built CoMFA (q2=0.595, r2=0.986, r2
pred =0.689) and CoMSIA (q2=0.762, r2=0.984,
r2
pred=0.822) models exhibited high robustness and prominent predicting ability. As revealed from
the results of molecular docking and molecular dynamics simulations, hydrogen bond and
hydrophobic interactions primarily impact the affinity of PAK4 inhibitors, and Leu398 acts as an
amino acid that leads to significant stabilization of the mentioned inhibitors. Moreover, the present
study developed five novel molecules exhibiting high biological activity predicted and satisfactory
ADME properties.

Conclusion:
The structural basis of PAK4 with respect to the activities of its inhibitors was revealed,
which may be conducive to designing novel PAK4 inhibitors.
A Comparative Effectiveness Systematic Review and Meta-analysis of
Drugs for the Prophylaxis of Junctional Ectopic Tachycardia
Authors: Mendel Brian , Christianto Christianto , Setiawan Moira , Prakoso Radityo , Siagian Sisca Natalia 
Published: June 2021

Background:
Junctional Ectopic Tachycardia (JET) is an arrhythmia originating from
the AV junction, which may occur following congenital heart surgery, especially when the intervention
is near the atrioventricular junction.

Objective:
The aim of this systematic review and meta-analysis is to compare the effectiveness of
amiodarone, dexmedetomidine, and magnesium in preventing JET following congenital heart
surgery.

Methods:
This meta-analysis was conducted according to the Preferred Reporting Items for Systematic
Review and Meta-Analysis (PRISMA) statement, where 11 electronic databases were searched
from the date of inception to August 2020. The incidence of JET was calculated with the relative
risk of 95% Confidence Interval (CI). Quality assessment of the included studies was assessed using
the Consolidated Standards of Reporting Trials (CONSORT) 2010 statement.

Results:
Eleven studies met the predetermined inclusion criteria and were included in this meta-analysis.
Amiodarone, dexmedetomidine, and magnesium significantly reduced the incidence of postoperative
JET [Amiodarone: risk ratio 0.34; I2= 0%; Z=3.66 (P=0.0002); 95% CI 0.19-0.60.
Dexmedetomidine: risk ratio 0.34; I2= 0%; Z=4.77 (P<0.00001); 95% CI 0.21-0.52. Magnesium:
risk ratio 0.50; I2= 24%; Z=5.08 (P<0.00001); 95% CI 0.39-0.66].

Conclusion:
All three drugs have shown promising results in reducing the incidence of JET. Our
systematic review found that dexmedetomidine is better in reducing the length of ICU stays as well
as mortality. In addition, dexmedetomidine also has the least pronounced side effects among the
three. However, it should be noted that this conclusion was derived from studies with small sample
sizes. Therefore, dexmedetomidine may be considered as the drug of choice for preventing JET.
Single-molecule Force Microscopy: A Powerful Tool for Studying the
Mechanical Properties of Cell Membranes
Authors: Shi Yan , Cai Mingjun , Wang Hongda 
Published: June 2021

Background:
Cell membrane is a physical barrier for cells, as well as an important
structure with complex functions in cell activities. The cell membrane can not only receive external
mechanical signal stimulation and make response (e.g. cell migration, differentiation, tumorigenesis,
growth), but it can also spontaneously exert force on the environment to regulate cell activities
(such as tissue repair, tumor metastasis, extracellular matrix regulation, etc.).

Methods:
This review provides the introduction of single-molecule force methods, as atomic
force microscopy, optical tweezers, magnetic tweezers, micropipette adhesion assay, tension
gauge tethers and traction force microscopy.

Results:
This review summarizes the principles, advantages and disadvantages of single-molecule
force methods developed in recent years as well as their application in terms of force received
and generated by cells. The study of cell mechanics enables us to understand the nature of mechanical
signal transduction and the manifestation of the cell's own movement.

Conclusion:
The study of the mechanical properties of cell microenvironment leads to a gradual
understanding of the important role of cell mechanics in development, physiology and pathology.
Recently developed combined methods are beneficial to further study of cell mechanics. The optimization
of these methods and the invention of new methods enable the continuing research on
cell mechanics.
Excellent Eco-friendly Selective Alcohols Oxidation by an Acid Functionalized
Imidazolium Based Ionic Liquid
Authors: Karthikeyan Parasuraman , Deepa Manickam , Uthayanila Selvarasu , Ganesh Gopalsamy Selvaraj , Priya Ramasamy Shanmuga 
Published: June 2021

Aims:
A green route for the oxidation of alcohols to corresponding carbonyl compounds in room temperature ionic liquid ([CEMIM]BH4) was developed by using hydrogen peroxide as the oxygen source. In aqueous solution at room temperature, 0.2 mol% of ([CEMIM]BH4) showed excellent catalytic properties for selective oxidation of aromatic and aliphatic alcohols

Background:
One of the vital reactions in organic synthesis is the oxidation of alcohols to carbonyl compounds. In particular, the conversion of primary alcohols to aldehydes has received a variety of applications as they are used as intermediates in fine chemicals mostly for the perfume industry.

Objective:
In the present work, we have reported an effective green route for the selective oxidation of alcohols to the carbonyl compounds using peroxide in an ionic liquid 1-carboxyethyl-3-methyl-imidazolium tetrahydroborate ([CEMIM]BH4)

Methods::
A mixture of alcohol (2 mmol), ([CEMIM]BH4) (0.2 mol%), H2O2 (2 mmol) were stirred thoroughly with the help of a magnetic stirrer for 10 min at ambient temperature

Results:
The catalytic activity of ([CEMIM]BH4) is very effective, which reflects its good solvating nature during the oxidation.

Conclusion:
In conclusion, the series of experiments described represents a useful method for the oxidation of primary and secondary alcohols to carbonyl compounds at room temperature. The catalyst can be easily prepared and is therefore extremely cost-effective. The rapid reaction times for the substrates mean a large number of materials may be screened in parallel over a short period of time.
The Art Of Social Work Practices In Indonesia The Impact of LSSR Policy on the Socio-Economic Sector in Banten Province
Authors: Amin Muhammad , Samputra Palupi Lindasari 
Published: June 2021

The Covid-19 pandemic is attacking the world, and measures are being taken to control the virus’s spread. Banten’s government is prohibited from enforcing the LSSR policy, which is based on Governor of Banten Decree 443 / Kep. 140-Huk / 2020 on the Establishment of Large-Scale Social Boundaries. This research employed quantitative descriptive method to determine if the LSSR impacts reducing the spread of the Covid-19 virus, as well as on the community’s social and economic well-being. The results indicated that unemployment would rise to 172 thousand by 2020. The poverty rate increased by 134.57 thousand. Income per capita decreases to 11,994 from 12,267 in 2019. The Human Development Index, which experienced a slowdown in growth in 2020, increased 0.01 points from 0.49 points the previous year. With an improvement of 0.15 points in the total length of schooling, it is greater than the 0.12point increase in 2019. The study recommends that the LSSR policy be maintained in order to prevent the spread of the Covid-19 virus, and that the government undertake fiscal stimulus efforts to improve the sustainability of micro, small, and medium-sized enterprises.
BURUH TANI JEMPUTAN DI DESA SAKO DUA, KEC. KAYU ARO BARAT, KAB. KERINCI, JAMBI
Authors: Wijaya Wibi , Zusmelia Zusmelia , Elvawati Elvawati 
Published: June 2021

Peasant pick up are peasant who do not work everyday but they are such kind of workers which is need to be called or picked up first for working. The purpose of this research is to see the factors causing the increase number of peasant pickup in community Sako Dua village Kayu Aro Barat district Kerinci Jambi. This research used qualitative approach with descriptive type. The informant is call peasant lanor and the owner of the field. Informan choosing with purposive sampling. Data Collected through observation (non-participant) and deep interview. Based on the result of the research it can be conclude that the factors causing the increase number of peasant pickup in community Sako Dua village is caused by internal factors and external factor from the peasant pickup themselves. Internal factors from peasant pickup such as 1). Economic Condition, 2). PTPN 6 Kayu Aro Retire influence, 3). Do not have agricultural land, 4). Do not have capital for cultivation, 5). Limited Job opportunity in the village. External factors from peasant pickup such as 1). The occurance of Patron-klien relationship in society of Sako Dua village with the owner of fields, 2). Less of power in managing the land.Buruh tani jemputan merupakan buruh tani yang tidak bekerja setiap hari melainkan buruh yang harus dipanggil atau dijemput terlebih dahulu untuk bekerja. Penelitian ini bertujuan untuk melihat faktor penyebab meningkatnya jumlah buruh tani jemputan dalam kehidupan masyarakat Desa Sako Dua Kecamatan Kayu Aro Barat Kabupaten Kerinci Jambi.Penelitian ini menggunakan pendekatan kualitatif dengan tipe deskriptif. Informan penelitian ini adalah buruh tani jemputan dan pemilik ladang. Pemilihan informan menggunakan teknik purposive sampling pengumpulan data dilakukan melalui observasi (non-participant), wawancara mendalam. Penelitian menunjukkan bahwa faktor penyebab meningkatnya jumlah buruh tani jemputan di Desa Sako Dua karena faktor internal dan eksternal dari buruh tani jemputan. Faktor internal dari buruh tani jemputan yaitu 1). Keadaan Ekonomi, 2). Pengaruh pensiunan PTPN 6 Kayu Aro, 3). Tidak memiliki lahan pertanian, 4). Tidak memiliki modal untuk mengolah lahan, 5). Terbatasnya lapangan pekerjaan di desa. Faktor eksternal dari buruh tani jemputan adalah 1). Munculnya hubungan patron-klien dalam masyarakat Desa Sako Dua dengan pemilik ladang, 2). Kurangnya tenaga dalam mengolah lahan.
KONFLIK PENGELOLAAN PARKIR LIAR DI PANTAI PURUS, KEC. PADANG BARAT, KOTA PADANG
Authors: Amril Ilmiati , Abbas Ardi , Prahara Surya 
Published: June 2021

This article aim to describe the conflict of illegal parking management ini Purus beach, Padang.. Research conducted with qualitative approach through descriptive type. Informants selected with purposive sampling. Data collected throught partisipative observation, indeepth interview and study document. The result is illegal parking in Purus started since 2008 and growing in 2013. Conlict is between illegal parking attendants and the owner of the vehicle, where the vehicle owner loses something when parking, conflict is between illegal parking attendant and UPT parking in the process of demolition. Conflict resolution between between illegal parking attendant and the owner of the vehicle is throught conciliation and conflict resolution between UPT parking with illegal parking attendants thrught pursuing cooperation strategy Penelitian ini bertujuan untuk mendeskripsikan konflik pengelolaan parkir liar di Purus Padang. Pendekatan yang digunakan dalam penelitian ini adalah kualitatif dengan tipe deskriptif analisis. Pemilihan informan mengggunakan teknik purpossive sampling. Metode yang digunakan untuk pengumpulan data dilakukan dengan cara observasi berperan serta terbatas, wawancara mendalam (Indepth Interview) dan studi dokumen. Hasil penelitian menunjukkan bahwa munculnya parkir liar di Pantai Purus berawal semenjak jembatan penghubung dibangun pada tahun 2008 dan berkembang pada tahun 2013. Bentuk konflik yang terjadi dalam pengelolaan parkir liar adalah konflik antara petugas parkir liar dengan pemilik kendaraan, dimana pemilik kendaraan kehilangan barangnya disaat parkir, lalu konflik petugas parkir liar dengan UPT perparkiran dalam proses penertiban. Upaya penyelesaian konflik antara petugas parkir liar dengan pemilik kendaraan dengan cara konsiliasi dan upaya penyelesaian konflik petugas parkir liar dengan UPT Perparkiran dengan melakukan strategi kooperasi
Konflik Tanah Ulayat Antara Kaum Caniago Di Nagari Kasang Dengan Badan Pertanahan Nasional Padang Pariman
Authors: Fitlayeni Rinel 
Published: June 2021

Communal land at the Minangkabau community identity and are protected by the Government contained in the UUPA. In defending existence, no wonder the increased intensity of conflict in society, even the biggest contributor in the court case is the problem of communal land. The conflict not only involve the public but also among the public with the state caused due to the interest of both parties . This paper wants to describe the conflict between members of the Caniago with BPN Padang Pariaman district. Conflicts involving both groups has occurred since 2002 and even up to now still continue.Tanah ulayat di Minangkabau merupakan identitas masyarakat dan dilindungi keberadaannya oleh negara yang tertuang dalam UUPA. Dalam mempertahankan kebedaraannya, tidak heran terjadi peningkatan intensitas konflik di tengah masyarakat, bahkan penyumbang perkara terbesar di pengadilan adalah permasalahan tanah ulayat. Konflik yang terjadi bukan saja melibatkan antar masyarakat tetapi juga masyarakat dengan negara yang disebabkan karena faktor kepentingan kedua belah pihak.. Tulisan ini ingin mendeskripsikan konflik antara anggota kaum Caniago dengan BPN Kabupaten Padang Pariaman. Konflik yang melibatkan kedua belah kelompok sudah terjadi sejak tahun 2002 bahkan sampai sekarang.
Analisis Pemenuhan Hak Dasar Anak Pada Program “Kota Layak Anak” Di Kecamatan Gading Cempaka, Bengkulu
Authors: Himawati Ika Pasca , Nopianti Heni , Hartati Sri , Hanum Sri Handayani 
Published: June 2021

The purpose of this research is to find and to analyzes the fulfillment of the basic rights on child based on the regulation of the state minister for women empowerment and child protection of the republic of Indonesia No. 12 of 2011 on indicators district of a city worthy of child. The research was done in 2 areas which is located in Gading Cempaka Subdistrict, they are in Cempaka Permai and Lingkar Baratvillage. Research conducted with qualitative approach and data was collected throughout observation, interview , FGD and study document . The result is a). In the both of areas have not had children forum which can directly accommodate the aspirations of children and do not involve children (age category of teenagers) on the activities and deliberations or work programs that exist in the environment RT or RW. b). In the both of areas has not been in the region of the unavailability of two consulting agencies for parents/family and child welfare agencies. c). In the both of areas has not been in an optimum manner use of leisure time and cultural activities it was found problems yet the number of program activity level of RT and RW aimed at maximizing the potential of children, as well as the unavailability of Green Open Space (RTH) as playing area that is safe and comfortable for children. Tujuan penelitian ini ialah menemukenali serta menganalisis pemenuhan hak dasar pada anak yang didasarkan pada Peraturan Menteri Negara Pemberdayaan Perempuandan Perlindungan Anak Republik Indonesia No. 12 Tahun 2011 tentang Indikator Kabupaten Kota Layak Anak. Penelitian dilakukan di 2 kawasan yang berada di Kecamatan Gading Cempaka, yakni Kelurahan Cempaka Permai dan Kelurahan Lingkar Barat. Peneliti menggunakan pendekatan kualitatif dengan teknik pengambilan informan melalui purposive dan snowball sampling. Adapun teknik pengambilan data dilakukan melalui observasi, wawancara, FGD dan studi dokumen. Temua penelitian menunjukkan bahwa a). Kedua wilayah penelitian belum memiliki forum anak yang dapat mengakomodir aspirasi anak secara langsung serta belum melibatkan anak khususnya anak kategori usia remaja pada kegiatan dan musyawarah ataupun program kerja yang ada di lingkungan RT/RW maupun kelurahan, b). Di dua kawasan tersebut belum tersedia lembaga konsultasi bagi orang tua/keluarga dan lembaga kesejahteraan anak. c). Belum banyaknya program kegiatan di tingkat RT dan RW yang ditujukan untuk memaksimalkan potensi anak serta belum tersedianya kawasan Ruang terbuka Hijau (RTH) sebagai kawasan bermain yang amandan nyaman bagi anak.