scholarly journals Chemical Synthesis, Efficacy and Safety of Antimalarial Hybrid Drug Comprising of Sarcosine and Aniline Pharmacophores as Scaffolds

Author(s):  
Jean Baptiste Niyibizi ◽  
Peter G. Kirira ◽  
Francis T. Kimani ◽  
Fiona Oyatsi ◽  
Joseph K. Ng’ang’a

Background: Reducing the impact of malaria is a key to achieving the sustainable development goals which are geared towards eradicating the disease. The main objective of this study was to synthesize, determine the efficacy and safety of antiplasmodial hybrid drug comprising of sarcosine and aniline derivative for management of plasmodial infections. Results: The hybrid drug was synthesized by adding thionyl chloride to sarcosine in order to form acyl chloride which was then added to aniline to form sarcosine-aniline hybrid molecule. The IC50 of sarcosine-aniline hybrid was 44.80 ± 4.70 ng/ml compared to that of aniline derivative which was 22.86 ± 1.26 ng/ml. The IC50 of control drugs were 2.63 ± 0.38 ng/ml, 5.69 ± 0.39 ng/ml for artesunate and chloroquine respectively. There was a significant difference between IC50 of sarcosine-aniline hybrid and aniline derivative (P<0.05). There was also a significant difference between sarcosine-aniline hybrid and standard drugs used to treat malaria including artesunate and chloroquine (P<0.05). The ED50 of sarcosine-aniline hybrid drug was 6.49mg/kg compared to that of aniline derivative which was 3.61mg/kg. The ED50 of control drugs were 3.56 mg/kg, 2.94mg/kg and 1.78 mg/kg for artesunate-aniline hybrid, artesunate and chloroquine respectively. There was a significant difference (P<0.05) between ED50 of sarcosine-aniline hybrid and both controls such as aniline derivative, artesunate, artesunate-aniline hybrid and chloroquine. Cytotoxicity results revealed that sarcosine-aniline hybrid was safe to vero cells with a CC50 of 50.18±3.53µg/ml. Sarcosine-aniline hybrid was significantly less toxic compared to artesunate, chloroquine and doxorubicin. Sarcosine-aniline hybrid was also safe to mice. Conclusion: Therefore, covalent bitherapy should be used in drug development for drug resistance mitigation.

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Jean Baptiste Niyibizi ◽  
Peter G. Kirira ◽  
Francis T. Kimani ◽  
Fiona Oyatsi ◽  
Joseph K. Ng’ang’a

Malaria is a disease caused by protozoans transmitted to humans by infected female Anopheles mosquitoes. According to the WHO report of 2015, there were 214 million cases of malaria with 438,000 deaths worldwide. Ninety percent of world’s malaria cases occur in Africa, where the disease is recognized as a serious impediment to economic and social development. Despite advancement in malaria research, the disease continues to be a global problem, especially in developing countries. Currently, there is no effective vaccine for malaria control. In addition, although there are effective drugs for treatment of malaria, this could be lost to the drug resistance in different Plasmodium species. The most lethal form is caused by P. falciparum which has developed resistance to many chemotherapeutic agents and possibly to the current drugs of choice. Reducing the impact of malaria is a key to achieving the sustainable development goals which are geared toward combating the disease. Covalent bitherapy is a rational and logical way of drug design which entails joining a couple of molecules with individual intrinsic action into a unique agent, hence packaging dual activity into one hybrid. This suggests the need to develop new antimalarial drugs that are effective against malaria parasites based on the new mode of action, molecular targets, and chemical structures. In silico studies have shown that sarcosine is able to bind to unique plasmodia proteins (P. falciparum ATCase), whereas aniline can be a ligand to target protein (enoyl acyl carrier protein reductase), hence suppressing the progression of the disease. The main objective of this study was to synthesize and determine the efficacy and safety of antiplasmodial hybrid drug comprising the sarcosine and aniline derivative for management of plasmodial infections. The hybrid drug was synthesized by adding thionyl chloride to sarcosine to form acyl chloride which was then added to aniline to form sarcosine-aniline hybrid molecule. The IC50 of sarcosine-aniline hybrid was 44.80 ± 4.70 ng/ml compared with that of aniline derivative which was 22.86 ± 1.26 ng/ml. The IC50 of control drugs was 2.63 ± 0.38 ng/ml and 5.69 ± 0.39 ng/ml for artesunate and chloroquine, respectively. There was a significant difference between IC50 of sarcosine-aniline hybrid and aniline derivative (p<0.05). There was also a significant difference between sarcosine-aniline hybrid and standard drugs used to treat malaria including artesunate and chloroquine (p<0.05). The ED50 of sarcosine-aniline hybrid drug was 6.49 mg/kg compared with that of aniline derivative which was 3.61 mg/kg. The ED50 of control drugs was 3.56 mg/kg, 2.94 mg/kg, and 1.78 mg/kg for artesunate-aniline hybrid, artesunate, and chloroquine, respectively. There was a significant difference (p<0.05) between ED50 of sarcosine-aniline hybrid and both controls such as aniline derivative, artesunate, artesunate-aniline hybrid, and chloroquine. Cytotoxicity results revealed that sarcosine-aniline hybrid was safe to vero cells with a CC50 of 50.18 ± 3.53 μg/ml. Sarcosine-aniline hybrid was significantly less toxic compared with artesunate, chloroquine, and doxorubicin. Sarcosine-aniline hybrid was efficacious and safe to mice. Therefore, covalent bitherapy should be used in drug development for drug resistance mitigation.


2021 ◽  
Vol 13 (14) ◽  
pp. 7738
Author(s):  
Nicolás Gambetta ◽  
Fernando Azcárate-Llanes ◽  
Laura Sierra-García ◽  
María Antonia García-Benau

This study analyses the impact of Spanish financial institutions’ risk profile on their contribution to the 2030 Agenda. Financial institutions play a significant role in ensuring financial inclusion and sustainable economic growth and usually incorporate environmental and social considerations into their risk management systems. The results show that financial institutions with less capital risk, with lower management efficiency and with higher market risk usually make higher contributions to the Sustainable Development Goals (SDGs), according to their sustainability reports. The novel aspect of the present study is that it identifies the risk profile of financial institutions that incorporate sustainability into their business operations and measure the impact generated in the environment and in society. The study findings have important implications for shareholders, investors and analysts, according to the view that sustainability reporting is a vehicle that financial institutions use to express their commitment to the 2030 Agenda and to higher quality corporate reporting.


Author(s):  
Н.П. РЕЗНИКОВА ◽  
Г.С. АРТЕМЬЕВА ◽  
Д.В. КАЛЮГА

Представлены основные направления для поиска путей улучшения рейтинга Российской Федерации в международных статистических сопоставлениях в сфере электросвязи/ИКТ с учетом необходимости гармонизации разнообразных направлений деятельности, связанных с оценкой влияния электросвязи/ИКТ на достижение Целей устойчивого развития, а также с появлением Нового индекса Международного союза электросвязи (МСЭ) взамен Индекса развития ИКТ(IDI). OThe main directions for finding ways to improve the rating of the Russian Federation in international statistical comparisons in the field of telecommunications/ICT are presented, taking into account the need to harmonize various activities related to assessing the impact of telecommunications/ICTs on achieving the sustainable development goals, as well as the advent of the new International Telecommunication Union Index instead of the ICT Development Index (IDI).


Ekonomika APK ◽  
2021 ◽  
Vol 320 (6) ◽  
pp. 89-100
Author(s):  
Ihor Sabii

The purpose of the article is to assess the impact of existing legislative initiatives in the field of agricultural land turnover on the possibility of achieving the Sustainable Development Goals in Ukraine and the implementation of land management based on an inclusive model of sustainable rural development. Research methods. The following methods were used: dialectical methods of cognition of processes and phenomena; empirical method (based on a comprehensive assessment of the current state of regulation of land relations in agriculture); comparative analysis method; abstract-logical (theoretical generalizations and formulation of conclusions). Research results. Established in the process of analysis of laws and bills on land reform and regulation of market circulation of agricultural land, adopted and registered in the Verkhovna Rada of Ukraine during 2020 - the first half of 2021, their impact on the level of viability and competitiveness of individuals, farmers, family farms, small and medium-sized agricultural enterprises in the new legal and economic conditions. Scientific novelty. The influence of individual legislative initiatives in the field of agricultural land turnover on the possibility of achieving the Sustainable Development Goals in Ukraine and the introduction of land management based on an inclusive model of sustainable rural development has been determined. Practical significance. The calculation of the amount of the minimum tax liability (MTL) for each region of Ukraine, taking into account the normative monetary value of the arable land, was carried out and its impact on the economic situation of small and medium-sized agricultural producers was assessed. Figs.: 6. Refs.: 38.


2020 ◽  
Vol 12 (6) ◽  
pp. 679-689
Author(s):  
Carla Cardoso

Purpose At a time when tourism is embarking on the path to recovery from the COVID-19 crisis, this paper aims to put forward a set of principles guiding the development of tourism to enable global society to become more inclusive and sustainable. Design/methodology/approach This paper adopted a descriptive design using views and data mainly published by 11 international organisations and specialised agencies between March and mid-June 2020. Content analysis was carried out to enable the research to identify features and the presence of challenges for tourism within international organisations’ documents and leaders’ speeches to compare them. Findings The results revealed that there are five key principles that may have a significant impact on tourism development, suggesting that these could be adopted for building a more inclusive and sustainable economy, while mitigating the impact of the COVID-19 crisis. Practical implications Adopting the five key principles recommended in this paper can help tourism to emerge stronger and in a more sustainable way from COVID-19 or other future crises. Equally, this can incite changes in policies, business practices and consumers’ and locals’ behaviours with a view to building a truly sustainable sector. Originality/value This study helps to reconfirm existing knowledge in the COVID-19 context by highlighting five guiding principles that can help tourism players to respond to this crisis disruption and future ones via transformative innovation. In doing so, these will also be contributing to the achievement of the ideals and aims of the Sustainable Development Goals.


Author(s):  
Keith Nurse

Abstract Migration, diasporas and the growth of remittances are key contemporary development trends which impact directly the lives of one in seven persons and often some of the most vulnerable and as such are critical to achieving the Sustainable Development Goals and the 2030 Agenda of “leaving no one behind”. Migration is captured in four Goals and five Targets in the SDGs however it is argued that the developmental potential of migration for LDCs is an underexploited asset. The paper offers critical perspectives on the SDGs targets by analysing the impact of remittances (including South-South remittances) and other financial investments such as diaspora savings and bonds. The analysis then focusses on financial innovation through the growth of money transfer organizations in LDCs (i.e. Haiti, Tonga and Bangladesh) and the rise of mobile money. The impact of these trends on financial inclusion and the banking of unbanked populations is then considered. The paper concludes with some key recommendations and insights.


Materials ◽  
2021 ◽  
Vol 14 (24) ◽  
pp. 7638
Author(s):  
Dorin Maier

In order to reduce the impact of human activities on the environment, in 2015, the United Nations launched the 2030 Agenda for Sustainable Development, proposing 17 Sustainable Development Goals with 169 associated targets. It is well-known that the construction industry is a major contributor to global CO2 emissions, and if a solution to reduce construction activity is not possible, considering the increasing population, then other solutions must be developed to decrease their negative environmental impact. In this context, the purpose of this paper is to investigate whether the use of wood waste as a building material can be a solution to achieve the Sustainable Development Goals. The research procedure included a bibliometric literature search, a scientometric analysis and an in-depth discussion. The analysis was done with the help of the software VOSviewer and Bibliometrix; the data were extracted mainly from the ISI Web of Science database. The extraction of data was done using the PRISMA method, and thus a sample of 212 peer-reviewed journal articles was established. The main results indicate an increasing interest in this topic in the last several years, as well as a switch from considering wood waste as just a source to generate heat and energy to the use of wood waste as a building material. The main uses of wood waste as a building material are in the composition of particleboards and in various mortar and concrete mixtures. The field of wood waste has many potential directions towards future development, and if the immense treasure represented by the forests, and implicitly the wood, is used efficiently, it can be a good solution to the problem of sustainable development of society.


2021 ◽  
Vol 1 (516) ◽  
pp. 217-223
Author(s):  
O. O. Khandii ◽  
◽  
M. D. Kramchaninova ◽  
A. I. Liedovska ◽  
◽  
...  

The article explores the role and contribution of intellectual work to the process of ensuring and improving the main aspects of human life in accordance with the Global Sustainable Development Goals (SDGs). Intellectual work is considered as an important resource for the creation of high-quality, innovative production, which provides for solution of important global problems of sustainable development. As part of a multilateral integrated approach, the impact of intellectual work results on the achievements of SDGs is researched. It is determined that the SDGs are interconnected and reinforce each other in the process of achievement, which is why their results are also comprehensive, that is, the result of improvements in the field of one goal is the way to achieve another one. A reflection of the dominant role of intellectual work in achieving the Sustainable Development Goals is the ninth SDGs – innovation and infrastructure. The development of technologies, creation of innovations and breakthrough solutions are crucial in the context of achieving the SDGs, and, accordingly, intellectual work, intellectual property and innovations are increasingly becoming socially significant and, due to the increased importance, need developing and implementing the policy of the integrity of scientific research along with protecting their results. Prospect for further research in this direction can be the issues of enhancing the efficiency of intellectual workers and increasing the opportunities to use the potential of intellectual activity for the further development of society.


2021 ◽  
Vol 301 ◽  
pp. 03002
Author(s):  
Peter Čajka ◽  
Veronica Grebennikova ◽  
Hoang Manh Trung Vu ◽  
Van Tran Ngo

Our article tackles the timely and important issue of the university collaboration aimed at shaping up the sustainable urban areas and contributing to their development through the teaching and research. Universities provided qualified labour force, yield novel research solutions and act as hubs for entrepreneurial activity in urban areas. In this article, we show that even though most of the universities are concentrated in large urban centres and capital regions, many of them are located in small rural areas and have a profound effect on them. We also demonstrate the impact of universities on the sustainable development which is done through the sustainable education as well as the R&D approaches. These effects are very relevant for the co-designing of sustainable rural areas that can follow the principles of the United Nations’ Sustainable Development Goals and the green policies imposed by the majority of the local and central governments around the world.


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