Metal-Promoted Heterocyclization: A Heterosynthetic Approach to Face a Pandemic Crisis

The outbreak of SARS-CoV-2 has drastically changed our everyday life and the life of scientists from all over the world. In the last year, the scientific community has faced this worldwide threat using any tool available in order to find an effective response. The recent formulation, production, and ongoing administration of vaccines represent a starting point in the battle against SARS-CoV-2, but they cannot be the only aid available. In this regard, the use of drugs capable to mitigate and fight the virus is a crucial aspect of the pharmacological strategy. Among the plethora of approved drugs, a consistent element is a heterocyclic framework inside its skeleton. Heterocycles have played a pivotal role for decades in the pharmaceutical industry due to their high bioactivity derived from anticancer, antiviral, and anti-inflammatory capabilities. In this context, the development of new performing and sustainable synthetic strategies to obtain heterocyclic molecules has become a key focus of scientists. In this review, we present the recent trends in metal-promoted heterocyclization, and we focus our attention on the construction of heterocycles associated with the skeleton of drugs targeting SARS-CoV-2 coronavirus.

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God joins us in death

Review & Expositor ◽

10.1177/00346373211008850 ◽

2021 ◽

Vol 118 (1) ◽

pp. 42-53

Author(s):

Graham B. Walker

Keyword(s):

Scientific Community ◽

Religious Community ◽

Ecological Crisis ◽

Environmental Crisis ◽

The Earth ◽

Starting Point ◽

The World ◽

History Of ◽

Slow Violence ◽

Science And Faith

Graham B. Walker introduces the slow violence of the environmental crisis as a flashpoint in the question for the doctrine of providence in general and the history of the Cross specifically. Where is God in all this? Two immediate positions are identified: the first position assumes that God is located high above the world of chaos in the valley below. God intervenes as God deems appropriate. Questions of inordinate suffering challenge this starting point. A second notion begins in the chaotic valley below and asks, where is God in all of this? E. Frank Tupper begins in this valley and describes “the God of love (who) always does the most God can do.” Tupper identifies the ecological crisis as a significant factor in the chaos of human history. Walker amplifies this concern by introducing ecologist Rob Nixon’s critique of the Western addiction to global consumption and Edward O. Wilson’s appeal for the religious community and the scientific community to work together for the love of the earth. Looking for theological responses that unite both science and faith with a love for God’s world, Walker dialogues with Ian McFarland and Sallie McFague. Although McFarland and McFague start from divergent theological positions, they arrive at a similar conclusion: the self-limitation of human acquisitive desire for the love of God’s world and God’s identification with the suffering creation of the world in the death of Christ.

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Dreams Give Birth to Reality”. Engraving Austroseraphicum Coelum as an Attempt to Create a New Reality by the Spanish Habsburgs Dynastic Propaganda / Sny rodzą rzeczywistość…”. Grafika Austroseraphicum Coelum jako próba kreowania nowej rzeczywistości za pomocą propagandy dynastycznej Habsburgów hiszpańskich

Annales UMCS Sectio I (Filozofia Socjologia) ◽

10.2478/sectio-2013-0012 ◽

2014 ◽

Vol 39 (1) ◽

Author(s):

Jan Kurowiak

Keyword(s):

Seventeenth Century ◽

The Netherlands ◽

General Condition ◽

Symbolic System ◽

Political Situation ◽

Mission Of God ◽

Starting Point ◽

The World ◽

The Church

AbstractAs a work of propaganda, graphics Austroseraphicum Coelum Paulus Pontius should create a new reality, make appearances. The main impression while seeing the graphics is the admiration for the power of Habsburgs, which interacts with the power of the Mother of God. She, in turn, refers the viewer to God, as well as Franciscans placed on the graphic, they become a symbol of the Church. This is a starting point for further interpretation of the drawing. By the presence of certain characters, allegories, symbols, we can see references to a particular political situation in the Netherlands - the war with the northern provinces of Spain. The message of the graphic is: the Spanish Habsburgs, commissioned by the mission of God, they are able to fight all of the enemies, especially Protestants, with the help of Immaculate and the Franciscans. The main aim of the graphic is to convince the viewer that this will happen and to create in his mind a vision of the new reality. But Spain was in the seventeenth century nothing but a shadow of former itself (in the time of Philip IV the general condition of Spain get worse). That was the reason why they wanted to hold the belief that the empire continues unwavering. The form of this work (graphics), also allowed to export them around the world, and the ambiguity of the symbolic system, its contents relate to different contexts, and as a result, the Habsburgs, not only Spanish, they could promote their strength everywhere. Therefore it was used very well as a single work of propaganda, as well as a part of a broader campaign

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The International Action “Open Access Week — 2009”

Bibliotekovedenie [Library and Information Science (Russia)] ◽

10.25281/0869-608x-2009-0-5-97-98 ◽

2009 ◽

pp. 97-98

Author(s):

Yulia V. Samodova

Keyword(s):

Open Access ◽

Scientific Community ◽

International Scientific Community ◽

International Action ◽

The World

Information on the coming Open Access Week which will be held from 19 to 23 October 2009. Interest in the results of scientific researches all over the world has led to consolidation of forces of the international scientific community and to expand the now-annual event from a single day to seven days.

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The Paradox of “A High Standard of Public Honesty”

10.1093/oso/9780198809975.003.0015 ◽

2017 ◽

Author(s):

James Kennedy ◽

Ronald Kroeze

Keyword(s):

The Netherlands ◽

Early Modern ◽

Side Effect ◽

High Standard ◽

Dutch Republic ◽

Liberal Politics ◽

Patronage Politics ◽

Starting Point ◽

The World ◽

Late Nineteenth

This chapter takes as its starting point the contemporary idea that the Netherlands is one of the least corrupt countries in the world; an idea that it dates back to the late-nineteenth and early-twentieth centuries. In this chapter, the authors explain how corruption was controlled in the Netherlands against the background of the rise and fall of the Dutch Republic, modern statebuilding and liberal politics. However, the Dutch case also presents some complexities: first, the decrease in some forms of corruption was due not to early democratization or bureaucratization, but was rather a side-effect of elite patronage-politics; second, although some early modern forms of corruption disappeared around this period, new forms have emerged in more recent times.

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Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry

SLAS DISCOVERY Advancing Life Sciences ◽

10.1177/24725552211000652 ◽

2021 ◽

pp. 247255522110006

Author(s):

Lesley-Anne Pearson ◽

Charlotte J. Green ◽

De Lin ◽

Alain-Pierre Petit ◽

David W. Gray ◽

...

Keyword(s):

High Throughput ◽

High Throughput Screening ◽

Mutational Analysis ◽

Nonstructural Protein ◽

Translation Efficiency ◽

Screening Assay ◽

High Throughput Screening Assay ◽

Starting Point ◽

Approved Drugs ◽

High Throughput Assay

Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) represents a significant threat to human health. Despite its similarity to related coronaviruses, there are currently no specific treatments for COVID-19 infection, and therefore there is an urgent need to develop therapies for this and future coronavirus outbreaks. Formation of the cap at the 5′ end of viral RNA has been shown to help coronaviruses evade host defenses. Nonstructural protein 14 (nsp14) is responsible for N7-methylation of the cap guanosine in coronaviruses. This enzyme is highly conserved among coronaviruses and is a bifunctional protein with both N7-methyltransferase and 3′-5′ exonuclease activities that distinguish nsp14 from its human equivalent. Mutational analysis of SARS-CoV nsp14 highlighted its role in viral replication and translation efficiency of the viral genome. In this paper, we describe the characterization and development of a high-throughput assay for nsp14 utilizing RapidFire technology. The assay has been used to screen a library of 1771 Food and Drug Administration (FDA)-approved drugs. From this, we have validated nitazoxanide as a selective inhibitor of the methyltransferase activity of nsp14. Although modestly active, this compound could serve as a starting point for further optimization.

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One-Shot Fabrication of Polymeric Hollow Microneedles by Standard Photolithography

Polymers ◽

10.3390/polym13040520 ◽

2021 ◽

Vol 13 (4) ◽

pp. 520 ◽

Cited By ~ 2

Author(s):

Principia Dardano ◽

Selene De Martino ◽

Mario Battisti ◽

Bruno Miranda ◽

Ilaria Rea ◽

...

Keyword(s):

Light Propagation ◽

World Market ◽

Emerging Technology ◽

Standard Formulation ◽

Proof Of Concept ◽

Fabrication Technique ◽

The World ◽

Small Doses ◽

Approved Drugs ◽

Hollow Microneedles

Microneedles (MNs) are an emerging technology in pharmaceutics and biomedicine, and are ready to be commercialized in the world market. However, solid microneedles only allow small doses and time-limited administration rates. Moreover, some well-known and already approved drugs need to be re-formulated when supplied by MNs. Instead, hollow microneedles (HMNs) allow for rapid, painless self-administrable microinjection of drugs in their standard formulation. Furthermore, body fluids can be easily extracted for analysis by a reverse use of HMNs, thus making them perfect for sensing issues and theranostics applications. The fabrication of HMNs usually requires several many-step processes, increasing the costs and consequently decreasing the commercial interest. Photolithography is a well-known fabrication technique in microelectronics and microfluidics that fabricates MNs. In this paper, authors show a proof of concept of a patented, easy and one-shot fabrication of two kinds of HMNs: (1) Symmetric HMNs with a “volcano” shape, made by using a photolithographic mask with an array of transparent symmetric rings; and (2) asymmetric HMNs with an oblique aperture, like standard hypodermic steel needles, made by using an array of transparent asymmetric rings, defined by two circles, which centers are slightly mismatched. Simulation of light propagation, fabrication process, and preliminary results on ink microinjection are presented.

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The role of edible insects to mitigate challenges for sustainability

Open Agriculture ◽

10.1515/opag-2020-0206 ◽

2021 ◽

Vol 6 (1) ◽

pp. 24-36

Author(s):

Raquel P. F. Guiné ◽

Paula Correia ◽

Catarina Coelho ◽

Cristina A. Costa

Keyword(s):

Nutritional Value ◽

Animal Feed ◽

World Population ◽

Edible Insects ◽

Strong Component ◽

Human Food ◽

The World ◽

Food And Feed ◽

Recent Trends

Abstract This review is focused on the utilization of insects as a new opportunity in food and feed products, including their commercialization both in traditional and new markets. It has been suggested that insects are considerably more sustainable when compared with other sources of animal protein, thus alleviating the pressure over the environment and the planet facing the necessity to feed the world population, constantly increasing. Many chefs have adhered to the trend of using insects in their culinary preparations, bringing insects to the plan of top gastronomy, highlighting their organoleptic qualities allied to a recognized high nutritional value. However, in some markets, insects or insect-based products are not readily accepted because of neophobia and disgust. Moreover, the insect markets, farming, and commercialization are experiencing a huge growth, in which the domain of animal feed is undoubtedly a very strong component. The future of insects as human food and animal feed seems promising in view of the recent trends and challenges.

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Contracting in land and natural resources: a tale of exclusion

International Journal of Law in Context ◽

10.1017/s1744552321000094 ◽

2021 ◽

Vol 17 (1) ◽

pp. 145-153

Author(s):

Federica Violi

Keyword(s):

Natural Resources ◽

Large Scale ◽

Sustainable Development Goals ◽

Host Countries ◽

Developmental Needs ◽

Starting Point ◽

The World ◽

Development Goals ◽

Short Essay ◽

Public Environment

By browsing the website of Land Matrix, one can measure the extent of land-related large-scale investments in natural resources (LRINRs) and place it on the world map. At the time of writing, the extent of these investments covers an area equal to the surfaces of Spain and Portugal together – or, for football fans, around 60 million football pitches. These investment operations have often been saluted as instrumental to achieve the developmental needs of host countries and as the necessary private counterpart to state (and interstate) efforts aimed at (sustainable) development goals. Yet, the realities on the ground offer a scenario characterised by severe instances of displacement of indigenous or local communities and environmental disruptions. The starting point of this short essay is that these ‘externalities’ are generated through the legal construct enabling the implementation of these investment operations. As such, this contribution lies neatly in the line of research set forth in the excellent books of Kinnari Bhatt and Jennifer Lander, from the perspective of both the development culture shaping these investment operations and the private–public environment in which these are situated. The essay tries and dialogues with both components, while focusing at a metalevel on the theoretical shifts potentially geared to turn a ‘tale of exclusion’ into a ‘tale of inclusion’.

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Challenges and Prospects of Using Treated Wastewater to Manage Water Scarcity Crises in the Gulf Cooperation Council (GCC) Countries

Water ◽

10.3390/w12071971 ◽

2020 ◽

Vol 12 (7) ◽

pp. 1971

Author(s):

Asad Sarwar Qureshi

Keyword(s):

Sustainable Use ◽

Integrated Approach ◽

Gulf Cooperation Council ◽

Treated Wastewater ◽

Regional Security ◽

Forage Crops ◽

Effective Response ◽

Groundwater Levels ◽

Gcc Countries ◽

The World

The Gulf Cooperation Council (GCC) countries are located in the driest part of the world with an annual per capita water availability of 500 m3 compared to the world average of 6000 m3. Agricultural water demand, which is more than 80% of the total water consumption, is primarily met through the massive exploitation of groundwater. The enormous imbalance between groundwater discharge (27.8 billion m3) and recharge (5.3 billion m3) is causing the excessive lowering of groundwater levels. Therefore, GCC countries are investing heavily in the production of nonconventional water resources such as desalination of seawater and treated wastewater. Currently, 439 desalination plants are annually producing 5.75 billion m3 of desalinated water in the GCC countries. The annual wastewater collection is about 4.0 billion m3, of which 73% is treated with the help of 300 wastewater treatment plants. Despite extreme water poverty, only 39% of the treated wastewater is reused, and the remaining is discharged into the sea. The treated wastewater (TWW) is used for the landscape, forestry, and construction industries. However, its reuse to irrigate food and forage crops is restricted due to health, social, religious, and environmental concerns. Substantial research evidence exists that treated wastewater can safely be used to grow food and forage crops under the agroclimatic conditions of the GCC countries by adopting appropriate management measures. Therefore, GCC countries should work on increasing the use of TWW in the agriculture sector. Increased use of TWW in agriculture can significantly reduce the pressure on freshwater resources. For this purpose, a comprehensive awareness campaign needs to be initiated to address the social and religious concerns of farming communities and consumers. Several internal and external risks can jeopardize the sustainable use of treated wastewater in the GCC countries. These include climate change, increasing costs, technological and market-driven changes, and regional security issues. Therefore, effective response mechanisms should be developed to mitigate future risks and threats. For this purpose, an integrated approach involving all concerned local and regional stakeholders needs to be adopted.

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The river fans out: Chinese fiction since the late 1970s

European Review ◽

10.1017/s1062798703000206 ◽

2003 ◽

Vol 11 (2) ◽

pp. 193-208 ◽

Cited By ~ 1

Author(s):

HENRY Y. H. ZHAO

Keyword(s):

Western China ◽

Political Struggle ◽

Religious Consciousness ◽

Chinese Fiction ◽

The World ◽

Recent Trends ◽

Art For Art's Sake ◽

Artistic Quality ◽

Scholarly Attention ◽

Mao Era

The 25 years of the post-Mao era of Chinese fiction is divided into two distinct stages: the pre-1989 period, and the post-1989 period. If this division is true about almost everything else in China, it is especially true with literature. This is because literature had been used as a lethal weapon for political struggle by Mao before and during his regime, and this tradition, though strongly challenged in the post-Mao era, still lingers, though in very different forms now and much watered down. Even the recent trends of art for art's sake, or for the sake of entertainment, or for the sake of religious consciousness, could also be read as political gestures, and are indeed treated as such by Chinese literary officialdom, and also by Western China experts. Despite the fact that Chinese fiction has been highly politicized, this paper will examine, as much as possible, the development of fiction as an art. Only the artistic quality can support my argument that recent novels from China deserve not only more scholarly attention but also more reader appreciation than they have hitherto received around the world.

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