In searchof the potenttherapeutic agent as an α-glucosidase inhibitor, we have synthesized twenty-five analogs (1-25) of quinoline-based Schiff bases as an inhibitoragainst α-glucosidase enzyme under positive control acarbose (IC50 = 38.45 ± 0.80 µM). From the activity profile it was foundthat analogs 1, 2, 3, 4, 11, 12 and 20with IC50values 12.40 ± 0.40, 9.40 ± 0.30, 14.10 ± 0.40, 6.20 ± 0.30, 14.40 ± 0.40, 7.40 ± 0.20 and 13.20 ± 0.40 µMrespectively showed most potent inhibition among the series even than standard drug acarbose (IC50 = 38.45 ± 0.80 µM). Here in the present study analog 4 (IC50 = 6.20 ± 0.30 µM) was found with many folds better α-glucosidase inhibitory activity than the reference drug. Eight analogs like 5, 7, 8, 16, 17, 22, 24 and 25 among the whole series displayed less than 50% inhibition. The substituents effects on phenyl ring thereby superficially established through SAR study. Binding interactions of analogs and the active site of ligands proteins were confirmed through molecular docking study. Spectroscopic techniques like 1H NMR, 13C NMR and ESIMS were used for characterization.
4-Thiazolidinone analogs 1-20 were synthesized, characterized by (1)H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65μM, if compared with standard thiourea having IC50 value of 21.25±0.15μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34±0.02, 14.62±0.03, 8.43±0.01, 7.3±0.04, 2.31±0.002, 5.75±0.003, 8.81±0.005, and 1.73±0.001μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies.
Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the urease inhibitory potential. For that purpose, benzimidazole analogues 1-19 were synthesized and screened for in vitro urease inhibitory potential. Structures of all synthetic analogues were deduced by different spectroscopic techniques. All analogues revealed inhibition potential with IC50 values of 0.90 ± 0.01 to 35.20 ± 1.10 μM, when compared with the standard thiourea (IC50 = 21.40 ± 0.21 μM). Limited SAR suggested that the variations in the inhibitory potentials of the analogues are the result of different substitutions on phenyl ring. In order to rationalize the binding interactions of most active compounds with the active site of urease enzyme, molecular docking study was conducted.
New triazinoindole bearing thiazole/oxazole analogues (1-21) were synthesized and characterized through spectroscopic techniques such as HREI-MS, 1H and 13C NMR. The configuration of compound 2i and 2k was confirmed through NOESY. All analogues were evaluated against α-amylase inhibitory potential. Among the synthesized analogues, compound 1h, 1i, 1j, 2a and 2f having IC50 values 1.80 ± 0.20, 1.90 ± 0.30, 1.2 ± 0.30, 1.2 ± 0.01 and 1.30 ± 0.20 μM respectively, showed excellent α-amylase inhibitory potential when compared with acarbose as standard (IC50 = 0.91 ± 0.20 µM). All other analogues showed good to moderate inhibitory potential. Structural activity relationship (SAR) has been established and binding interactions were confirmed through docking studies.
A series of twenty-six analogs of benzimidazole based oxadiazole have been synthesized and evaluated against alpha-glycosidase enzyme. Most the analogs showed excellent to good inhibitory potential. Among the screened analogs, analog 1, 2, 3 and 14 with IC50 values 4.6 ± 0.1, 9.50 ± 0.3, 2.6 ± 0.1 and 9.30 ± 0.4 µM respectively showedexcellent inhibitory potential than reference drug acarbose (IC50 = 38.45 ± 0.80 µM). Some of the analogs like 19, 21, 22 and 23 with methyl and methoxy substituent on phenyl ring show hydrophobic interaction and were found with no inhibitory potential. The binding interactions between synthesized analogs and ligands protein were confirmed through molecular docking study. Various spectroscopic techniques like 1H NMR, 13C NMR, and EI-MS were used for characterization of all synthesized analogs. These derivatives were synthesized by simple mode of synthesis like heterocyclic ring formation.
A new library of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives (1-23) were synthesized and characterized by EI-MS and 1H NMR, and screened for their α-amylase inhibitory activity. Out of twenty-three derivatives, two molecules 19 (IC50=0.38±0.82µM) and 23 (IC50=1.66±0.14µM), showed excellent activity whereas the remaining compounds, except 10 and 17, showed good to moderate inhibition in the range of IC50=1.77-2.98µM when compared with the standard acarbose (IC50=1.66±0.1µM). A plausible structure-activity relationship has also been presented. In addition, in silico studies was carried out in order to rationalize the binding interaction of compounds with the active site of enzyme.
Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50 = 2.20 ± 0.1to 88.60 ± 1.70 µM) when compared with standard drug acarbose (IC50 = 38.45 ± 0.80 µM). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.
Isoquinoline analogues (KA-1 to 16) have been synthesized and evaluated for their E. coli thymidine phosphorylase inhibitory activity. Except compound 11, all other analogs showed outstanding thymidine inhibitory potential ranging in between 4.40 ± 0.20 to 69.30 ± 1.80 µM when compared with standard drug 7-Deazaxanthine (IC50 = 38.68 ± 4.42 µM). Structure Activity Relationships has been established for all compounds, mainly based on substitution pattern on phenyl ring. All analogs were characterized by various spectroscopic techniques such as 1H NMR, 13C NMR and EI-MS. The binding interactions of isoquinoline analogues with the active site of TP enzyme, the molecular docking studies were performed. Furthermore, the angiogenic inhibitory potentials of isoquinoline analogues (KA-1-9, 14, 12 and 16) were determined in the presence of standard drug Dexamethasone based on percentage inhibitions at various concentrations. Herein this work analogue KA-12, 14 and 16 emerged with most potent angiogenic inhibitory potentials among the synthesized analogues.
Synthesis of quinoline analogs and their urease inhibitory activities with reference to the standard drug, thiourea (IC50 = 21.86 ± 0.40 µM) are presented in this study. The inhibitory activity range is (IC50 = 0.60 ± 0.01 to 24.10 ± 0.70 µM) which displayed that it is most potent class of urease inhibitor. Analog 1-9, and 11-13 emerged with many times greater antiurease potential than thiourea, in which analog 1, 2, 3, 4, 8, 9, and 11 (IC50 = 3.50 ± 0.10, 7.20 ± 0.20, 1.30 ± 0.10, 2.30 ± 0.10, 0.60 ± 0.01, 1.05 ± 0.10 and 2.60 ± 0.10 µM respectively) were appeared the most potent ones among the series. In this context, most potent analogs such as 1, 3, 4, 8, and 9 were further subjected for their in vitro antinematodal study against C. elegans to examine its cytotoxicity under positive control of standard drug, Levamisole. Consequently, the cytotoxicity profile displayed that analogs 3, 8, and 9 were found with minimum cytotoxic outline at higher concentration (500 µg/mL). All analogs were characterized through 1H NMR, 13C NMR and HR-EIMS. The protein-ligand binding interaction for most potent analogs was confirmed via molecular docking study.
The α-amylase acts as attractive target to treat type-2 diabetes mellitus. Therefore in discovering a small molecule as α-amylase inhibitor, we have synthesized benzofuran carbohydrazide analogs (1-25), characterized through different spectroscopic techniques such as 1HNMR and EI-MS. All screened analog shows good α-amylase inhibitory potentials with IC50 value ranging between 1.078±0.19 and 2.926±0.05µM when compared with acarbose having IC50=0.62±0.22µM. Only nine analogs among the series such as analogs 3, 5, 7, 8, 10, 12, 21, 23 and 24 exhibit good inhibitory potential with IC50 values 1.644±0.128, 1.078±0.19, 1.245±0.25, 1.843±0.19, 1.350±0.24, 1.629±0.015, 1.353±0.232, 1.359±0.119 and 1.488±0.07µM when compare with standard drug acarbose. All other analogs showed good to moderate α-amylase inhibitory potentials. The SAR study was conducted on the basis of substituent difference at the phenyl ring. The binding interaction between analogs and active site of enzyme was confirmed by docking studies.
The aim of this study is to examine the impact of air pollutants, including mono-nitrogen oxides (NOx), nitrous oxide (N2O), sulfur dioxide (SO2), carbon dioxide emissions (CO2), and greenhouse gas (GHG) emissions on ecological footprint, habitat area, food supply, and biodiversity in a panel of thirty-four developed and developing countries, over the period of 1995-2014. The results reveal that NOx and SO2 emissions both have a negative relationship with ecological footprints, while N2O emission and real GDP per capita have a direct relationship with ecological footprints. NOx has a positive relationship with forest area, per capita food supply and biological diversity while CO2 emission and GHG emission have a negative impact on food production. N2O has a positive impact on forest area and biodiversity, while SO2 emissions have a negative relationship with them. SO2 emission has a direct relationship with per capita food production, while GDP per capita significantly affected per capita food production and food supply variability across countries. The overall results reveal that SO2, CO2, and GHG emissions affected potential habitat area, while SO2 and GHG emissions affected the biodiversity index. Trade liberalization policies considerably affected the potential habitat area and biological diversity in a panel of countries.
The pro-poor growth and environmental sustainability are the twin agendas widely discussed in environmental science literature. The technology-embodied growth helps to attain both agendas through knowledge sharing and technology transfer, which trickle down to the poor income group and improve their living standards. Hence, the role of information and communication technologies (ICTs) is deemed crucial in boosting economic growth and is under deep consideration to establish its role in reducing poverty and environmental pollution. The current study examines the long-run relationship between ICTs, poverty reduction, and ecological degradation in Pakistan using time series data from 1975-2018. The short- and long-run parameter estimates were obtained through the Autoregressive Distributed Lag (ARDL) model for robust inferences. The results substantiate the inverted U-shaped Environmental Kuznets Curve relationship between income and emissions with a turning point at US$1000 in the short-run and US$800 in the long-run. The results confirmed the decisive intervention of ICTs factors in the poverty reduction, i.e., computer communications and mobile-telephone-broadband subscriptions support to reduce poverty incidence with the mediation of inbound FDI in a country. As far as income inequality is concerned, it shows that computer services support minimizing income inequality via a channel of high-technology exports in a country. The technology embodied emissions verified in the long-run, where mobile-telephone-broadband subscriptions increase carbon emissions. Finally, mobile-telephone-broadband subscriptions and inbound FDI both are significant contributors to amplify the country's economic growth. The results conclude that poverty reduction and environmental sustainability agenda are achieved by developing green ICT infrastructure in a country.
The objective of the study is to examine the impact of environmental indicators and air pollution on "health" and "wealth" for the low-income countries. The study used a number of promising variables including arable land, fossil fuel energy consumption, population density, and carbon dioxide emissions that simultaneously affect the health (i.e., health expenditures per capita) and wealth (i.e., GDP per capita) of the low-income countries. The general representation for low-income countries has shown by aggregate data that consist of 39 observations from the period of 1975-2013. The study decomposes the data set from different econometric tests for managing robust inferences. The study uses temporal forecasting for the health and wealth model by a vector error correction model (VECM) and an innovation accounting technique. The results show that environment and air pollution is the menace for low-income countries' health and wealth. Among environmental indicators, arable land has the largest variance to affect health and wealth for the next 10-year period, while air pollution exerts the least contribution to change health and wealth of low-income countries. These results indicate the prevalence of war situation, where environment and air pollution become visible like "gun" and "bullet" for low-income countries. There are required sound and effective macroeconomic policies to combat with the environmental evils that affect the health and wealth of the low-income countries.
This study aims to determine an interactive environmental model for economic growth that would be supported by the "sustainability principles" across the globe. The study examines the relationship between environmental pollutants (i.e., carbon dioxide emission, sulfur dioxide emission, mono-nitrogen oxide, and nitrous oxide emission); population growth; energy use; trade openness; per capita food production; and it's resulting impact on the real per capita GDP and sectoral growth (i.e., share of agriculture, industry, and services in GDP) in a panel of 34 high-income OECD, high-income non-OECD, and Europe and Central Asian countries, for the period of 1995-2014. The results of the panel fixed effect regression show that per capita GDP are influenced by sulfur dioxide emission, population growth, and per capita food production variability, while energy and trade openness significantly increases per capita income of the region. The results of the panel Seemingly Unrelated Regression (SUR) show that carbon dioxide emission significantly decreases the share of agriculture and industry in GDP, while it further supports the share of services sector to GDP. Both the sulfur dioxide and mono-nitrogen oxide emission decreases the share of services in GDP; nitrous oxide decreases the share of industry in GDP; while mono-nitrogen oxide supports the industrial activities. The following key growth-specific results has been obtained from the panel SUR estimation, i.e., (i) Both the food production per capita and trade openness significantly associated with the increasing share of agriculture, (ii) food production and energy use significantly increases the service sectors' productivity; (iii) food production decreases the industrial activities; (iv) trade openness decreases the share of services to GDP while it supports the industrial share to GDP; and finally, (v) energy demand decreases along with the increase agricultural share in the region. The results emphasize the need for an interactive environmental model that facilitates the process of sustainable development across the globe.
This study investigates the relationship between energy consumption and carbon dioxide emission in the causal framework, as the direction of causality remains has a significant policy implication for developed and developing countries. The study employed maximum entropy bootstrap (Meboot) approach to examine the causal nexus between energy consumption and carbon dioxide emission using bivariate as well as multivariate framework for Malaysia, over a period of 1975-2013. This is a unified approach without requiring the use of conventional techniques based on asymptotical theory such as testing for possible unit root and cointegration. In addition, it can be applied in the presence of non-stationary of any type including structural breaks without any type of data transformation to achieve stationary. Thus, it provides more reliable and robust inferences which are insensitive to time span as well as lag length used. The empirical results show that there is a unidirectional causality running from energy consumption to carbon emission both in the bivariate model and multivariate framework, while controlling for broad money supply and population density. The results indicate that Malaysia is an energy-dependent country and hence energy is stimulus to carbon emissions.
The objective of the study is to examine the relationship between air pollution, fossil fuel energy consumption, water resources, and natural resource rents in the panel of selected Asia-Pacific countries, over a period of 1975-2012. The study includes number of variables in the model for robust analysis. The results of cross-sectional analysis show that there is a significant relationship between air pollution, energy consumption, and water productivity in the individual countries of Asia-Pacific. However, the results of each country vary according to the time invariant shocks. For this purpose, the study employed the panel least square technique which includes the panel least square regression, panel fixed effect regression, and panel two-stage least square regression. In general, all the panel tests indicate that there is a significant and positive relationship between air pollution, energy consumption, and water resources in the region. The fossil fuel energy consumption has a major dominating impact on the changes in the air pollution in the region.
The objective of the study is to examine the relationship between environmental indicators and health expenditures in the panel of five selected Asian countries, over the period of 2000-2013. The study used panel cointegration technique for evaluating the nexus between environment and health in the region. The results show that energy demand, forest area, and GDP per unit use of energy have a significant and positive impact on increasing health expenditures in the region. These results have been confirmed by single equation panel cointegration estimators, i.e., fully modified ordinary least squares (FMOLS), dynamic OLS (DOLS), and canonical cointegrating regression (CCR) estimators. In addition, the study used robust least squares regression to confirm the generalizability of the results in Asian context. All these estimators indicate that environmental indicators escalate the health expenditures per capita in a region; therefore, Asian countries should have to upsurge health expenditures for safeguard from environmental evils in a region.
The objective of the study is to establish the link between air pollution, fossil fuel energy consumption, industrialization, alternative and nuclear energy, combustible renewable and wastes, urbanization, and resulting impact on health services in Malaysia. The study employed two-stage least square regression technique on the time series data from 1975 to 2012 to possibly minimize the problem of endogeniety in the health services model. The results in general show that air pollution and environmental indicators act as a strong contributor to influence Malaysian health services. Urbanization and nuclear energy consumption both significantly increases the life expectancy in Malaysia, while fertility rate decreases along with the increasing urbanization in a country. Fossil fuel energy consumption and industrialization both have an indirect relationship with the infant mortality rate, whereas, carbon dioxide emissions have a direct relationship with the sanitation facility in a country. The results conclude that balancing the air pollution, environment, and health services needs strong policy vistas on the end of the government officials.
Environmental quality indicators are crucial for responsive and cost-effective policies. The objective of the study is to examine the relationship between environmental quality indicators and financial development in Malaysia. For this purpose, the number of environmental quality indicators has been used, i.e., air pollution measured by carbon dioxide emissions, population density per square kilometer of land area, agricultural production measured by cereal production and livestock production, and energy resources considered by energy use and fossil fuel energy consumption, which placed an impact on the financial development of the country. The study used four main financial indicators, i.e., broad money supply (M2), domestic credit provided by the financial sector (DCFS), domestic credit to the private sector (DCPC), and inflation (CPI), which each financial indicator separately estimated with the environmental quality indicators, over a period of 1975-2013. The study used the generalized method of moments (GMM) technique to minimize the simultaneity from the model. The results show that carbon dioxide emissions exert the positive correlation with the M2, DCFC, and DCPC, while there is a negative correlation with the CPI. However, these results have been evaporated from the GMM estimates, where carbon emissions have no significant relationship with any of the four financial indicators in Malaysia. The GMM results show that population density has a negative relationship with the all four financial indicators; however, in case of M2, this relationship is insignificant to explain their result. Cereal production has a positive relationship with the DCPC, while there is a negative relationship with the CPI. Livestock production exerts the positive relationship with the all four financial indicators; however, this relationship with the CPI has a more elastic relationship, while the remaining relationship is less elastic with the three financial indicators in a country. Energy resources comprise energy use and fossil fuel energy consumption, both have distinct results with the financial indicators, as energy demand have a positive and significant relationship with the DCFC, DCPC, and CPI, while fossil fuel energy consumption have a negative relationship with these three financial indicators. The results of the study are of value to both environmentalists and policy makers.
The objective of the study is to evaluate socio-economic and environmental factors that influenced the United Nations healthcare sustainable agenda in a panel of 21 Asian and African countries. The results show that changes in price level (0.0062, p