Sustainable Synthesis of Guanidine Derivatives and Computational Assessment of their Antidiabetic Efficacy.

BACKGROUND: Type 2 Diabetes Mellitus (T2DM) represents a significant and pressing worldwide health concern, necessitating the quest for enhanced antidiabetic pharmaceuticals. Guanidine derivatives, notably metformin and buformin, have emerged as pivotal therapeutic agents for T2DM management. AIMS: The present study introduces an efficient one-pot synthesis method for the production of symmetrical guanidine compounds. METHODS: This synthesis involves the reaction of isothiocyanates with secondary amines, employing an environmentally friendly and recyclable reagent, tetrabutylphosphonium tribromide (TBPTB). RESULTS: A comprehensive assessment of the biological activity of the synthesized guanidine compounds, specifically in the context of T2DM, has been rigorously conducted. CONCLUSION: Additionally, computational analyses have unveiled their substantial potential as promising antidiabetic agents. Results highlight the relevance of these compounds in the ongoing pursuit of novel therapeutic solutions for T2DM.

Environmentally benign synthesis of unsymmetrical ureas and their evaluation as potential HIV-1 protease inhibitors via a computational approach.

The present work reports the cost-effective, high yielding and environmentally acceptable preparation of unsymmetrical ureas from thiocarbamate salts using sodium percarbonate as an oxidant. Efficacy of the unsymmetrical ureas as potential human immune deficiency virus (HIV-1) protease inhibitors has been evaluated via in silico approach. The results revealed interactions of the urea compounds at the active site of the enzyme with favorable binding affinities causing possible mutations hindering the functioning of the enzyme. Further computational assessment of IC50 using known references satisfactorily authenticated the inhibitory action of the selected compounds against HIV-1 protease. Added to the easy synthesis of the ureas following an environmentally benign protocol, this work may be a valuable addition to the ongoing search for drugs with better efficacy profiles and reduced toxicity against HIV.

Glycome Profiling and Bioprospecting Potential of the Himalayan Buddhist Handmade Paper of Tawang Region of Arunachal Pradesh.

The paper and pulp industry (PPI) is one of the largest industries that contribute to the growing economy of the world. While wood remains the primary raw material of the PPIs, the demand for paper has also grown alongside the expanding global population, leading to deforestation and ecological imbalance. Wood-based paper production is associated with enormous utilization of water resources and the release of different wastes and untreated sludge that degrades the quality of the environment and makes it unsafe for living creatures. In line with this, the indigenous handmade paper making from the bark of Daphne papyracea, Wall. ex G. Don by the Monpa tribe of Arunachal Pradesh, India is considered as a potential alternative to non-wood fiber. This study discusses the species distribution modeling of D. papyracea, community-based production of the paper, and glycome profiling of the paper by plant cell wall glycan-directed monoclonal antibodies. The algorithms used for ecological and geographical modeling indicated the maximum predictive distribution of the plant toward the western parts of Arunachal Pradesh. It was also found that the suitable distribution of D. papyracea was largely affected by the precipitation and temperature variables. Plant cell walls are primarily made up of cellulose, hemicellulose, lignin, pectin, and glycoproteins. Non-cellulosic cell wall glycans contribute significantly to various physical properties such as density, crystallinity, and tensile strength of plant cell walls. Therefore, a detailed analysis of non-cellulosic cell wall glycan through glycome profiling and glycosyl residue composition analysis is important for the polymeric composition and commercial processing of D. papyracea paper. ELISA-based glycome profiling results demonstrated that major classes of cell wall glycans such as xylan, arabinogalactans, and rhamnogalacturonan-I were present on D. papyracea paper. The presence of these polymers in the Himalayan Buddhist handmade paper of Arunachal Pradesh is correlated with its high tensile strength. The results of this study imply that non-cellulosic cell wall glycans are required for the production of high-quality paper. To summarize, immediate action is required to strengthen the centuries-old practice of handmade paper, which can be achieved through education, workshops, technical know-how, and effective marketing aid to entrepreneurs.

Monitoring land use land cover changes in the Eastern Himalayan landscape of Nagaland, Northeast India.

The escalating demand for anthropic needs and urban development has highlighted the importance of monitoring and change detection of land use land cover (LULC). With an increase in agricultural expansion and infrastructural development, every land surface on earth calls for a long-term investigation of land modification patterns and their underlying contributory factors. The present investigation monitors the LULC changes and assesses the process controls in Kohima and Dimapur districts of Nagaland, India. Currently, these two districts encompassing the main urban cities of the hilly state are experiencing rapid urbanization and unplanned developmental activities. Alike any other LULC changes observed in unplanned and developing cities, these districts are likely to face environmental degradation, and particularly, the occurrence of frequent landslides and flash floods. The study has three objectives-(i) LULC mapping of Kohima and Dimapur districts for three periods (1998, 2008, and 2018), (ii) comparative analysis of LULC change patterns in the two districts during the three epochs (1998-2008, 2008-2018, and 1998-2018), and (iii) assessment of the contributory factors. For the study, remotely sensed LANDSAT images (TM and OLI) in Geographical Information System (GIS) platform were utilized along with field surveys. Supervised classification technique was employed and four major LULC classes were identified using Landsat level-1 classification system. The overall accuracy of the classification varied between 91 and 98%. Results showed that Built Up areas have increased significantly in both the districts at the rate of 322.6 ha/year in Kohima and 301.9 ha/year in Dimapur during 1998-2018. On the other hand, Agricultural Land and Forest Land declined in both districts. Changes in LULC were mainly due to marginalization of shifting cultivation, deforestation, infrastructural development, urban migration, and flourishing of aquaculture farming. This study furnishes baseline information on LULC in the data-scarce region of Northeast India and is an insinuation to the policy-makers to ensure sustainable land use planning in the face of rapid urbanization.