Benzotriazole-Mediated Facile Synthesis of Novel Glycosyl Tetrazole

A facile, simple, and high-yielding synthetic protocol for novel glycosyl tetrazoles has been devised from different carbohydrate-containing amides using benzotriazole methodology under mild reaction condition.     

Enzyme mediated synthesis of Ag–TiO2 photocatalyst for visible light degradation of reactive dye from aqueous solution

The purpose of this study was to develop bio-inspired photocatalyst with solar light activity for textile dye degradation. Three TiO₂ samples namely TiO₂ (TiO₂-A), biotemplated TiO₂ (TiO₂-B), and enzyme mediated Ag–TiO₂ biotemplate (TiO₂-C), were developed. The presence of anatase phase of TiO₂ and silver in synthesized samples were confirmed using X-ray diffraction, field emission scanning electron microscopy, energy-dispersive spectroscopy, and UV–Vis–NIR spectroscopy. Photocatalytic efficiencies of these photocatalysts were evaluated by studying the oxidation of a commercial reactive dye (reactive black) under solar light irradiation in batch reactors. Photocatalytic efficiencies of the sample were compared using statistical tools like one-way ANOVA and Tukey test. The results confirmed that photocatalytic efficiency of TiO₂-C was 40 % higher than that of TiO₂-A under solar light irradiation.     

First Synthesis of N‐Substituted Amino and N‐Sulfonylaminated Methylthiopyrimidines: Reaction of Dimethyl N‐Cyanodithioiminocarbonate With Substituted Hydrazides

A novel and efficient method for the synthesis of a new variety of methylsulfanylpyrimidines by the reaction of dimethyl N‐cyanodithioiminocarbonate with substituted hydrazides. The synthetic potential of the method is demonstrated.     

Grafting onto Wool. IX. Graft Copolymerization of Vinyl Monomers by Use of Vanadium Oxyacetylacetonate as Initiator

Methyl methacrylate (MMA), acrylic acid (AAc), and vinyl acetate (VAc) were graft copolymerized onto Himachali wool in an aqueous medium by using vanadium oxyacetyl acetonate as initiator. Graft copolymerization was studied at 45, 55, 65, and 75°C for various reaction periods. The percentage of grafting was determined as functions of concentration of monomers, concentration of initiator, time, and temperature. The maximum percentage of grafting with each monomer occurred at 55°. Several grafting experiments were carried out in the presence of various additives which include HNO3, DMSO, and pyridine. Nitric acid was found to promote grafting of MMA. All these additives had adverse effects on grafting of VAc and AAc. MMA, VAc, and AAc were found to differ in reactivity toward grafting and followed the order MMA > AAc > VAc.     

Urease Inhibitory Kinetic Studies of Various Extracts and Pure Compounds from Cinnamomum Genus

Urease is an enzyme that plays a significant role in the hydrolysis of urea into carbonic acid and ammonia via the carbamic acid formation. The resultant increase in pH leads to the onset of various pathologies such as gastric cancer, urolithiasis, hepatic coma, hepatic encephalopathy, duodenal ulcers and peptic ulcers. Urease inhibitors can reduce the urea hydrolysis rate and development of various diseases. The Cinnamomum genus is used in a large number of traditional medicines. It is well established that stem bark of Cinnamomum cassia exhibits antiulcerogenic potential. The present study evaluated the inhibitory effect of seven extracts of Cinnamomum camphora, Cinnamomum verum and two pure compounds Camphene and Cuminaldehyde on urease enzyme. Kinetic studies of potential inhibitors were carried out. Methanol extract (IC₅₀ 980 µg/mL) of C. camphora and a monoterpene Camphene (IC₅₀ 0.147 µg/mL) possess significant inhibitory activity. The Lineweaver Burk plot analysis suggested the competitive inhibition by methanol extract, hexane fraction and Camphene. The Gas Chromatography-Mass Spectroscopy (GC–MS) analysis of hexane fraction revealed the contribution of various terpenes. The present study targets terpenes as a new class of inhibitors that have potential therapeutic value for further development as novel drugs.     

Ultrasonic and Volumetric Study of N–H Bond Complexes in Binary Mixtures

Experimental values of the density and ultrasonic velocity have been measured for binary mixtures of butylamine with 1-butanol and with tert-butanol at temperatures of 293.15, 303.15 and 313.15 K over the entire mole fraction range. From these data, the excess molar volumes, deviations in isentropic compressibility, excess internal pressures, and excess molar enthalpies have been calculated. All of the excess functions were fitted to Redlich-Kister polynomial relations to estimate the adjustable parameters along with the standard deviations of the fits. The variations of these excess functions with mole fraction of butylamine have been examined. The changes in these parameters with composition suggest that the interaction between butylamine and 1-butanol is strong, whereas its interaction with tert-butanol is weak. Further, the partial molar volumes and partial molar compressibilities at infinite dilution have also been evaluated since these parameters provide better insight for studying intermolecular interactions.     

Flexible organic crystals. Understanding the tractable co-existence of elastic and plastic bending

As an emerging class of flexible materials, mechanically bendable molecular crystals are broadly classified as elastic or plastic. Nevertheless, flexible organic crystals with mutually exclusive elastic and plastic traits, with contrasting structural requirements, co-existing under different stress settings are exceptional; hence, it is imperative to establish the concurring factors that beget this rare occurrence. We report a series of halogen-substituted benzil crystals showing elastic bending (within ∼2.45% strain), followed by elastoplastic deformation under ambient conditions. Under higher stress settings, they display exceptional plastic flexibility that one could bend, twist, or even coil around a capillary tube. X-ray diffraction, microscopy, and computational data reveal the microscopic and macroscopic basis for the exciting co-existence of elastic, elastoplastic, and plastic properties in the crystals. The layered molecular arrangement and the weak dispersive interactions sustaining the interlayer region provide considerable tolerance towards breaking and making upon engaging or releasing the external stress; it enables restoring the original state within the elastic strain. Comparative studies with oxalate compounds, wherein the twisted diketo moiety in benzil was replaced with a rigid and coplanar central oxalate moiety, enabled us to understand the effect of the anisotropy factor on the crystal packing induced by the C O⋯C tetral interactions. The enhanced anisotropy depreciated the elastic domain, making the oxalate crystals more prone to plastic deformation. Three-point bending experiments and the determined Young''s moduli further corroborate the co-existence of the elastic and plastic realm and highlight the critical role of the underlying structural elements that determine the elastic to plastic transformation. The work highlights the possible co-existence of orthogonal mechanical characteristics in molecular crystals and further construed the concurrent role of microscopic and macroscopic elements in attaining this exceptional mechanical trait.

Structural and mechanical studies of benzil and oxalate crystals highlight the microscopic and macroscopic basis for the co-existence of orthogonal mechanical traits and the elastic to plastic transformation under different stress settings.     

Tirzepatide,a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

The prevalence of obesity and diabetes is an increasing global problem, especially in developed countries, and is referred to as the twin epidemics. As such, advanced treatment approaches are needed. Tirzepatide, known as a ‘twincretin’, is a ‘first-in-class’ and the only dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) receptor agonist, that can significantly reduce glycemic levels and improve insulin sensitivity, as well as reducing body weight by more than 20% and improving lipid metabolism. This novel anti-diabetic drug is a synthetic peptide analog of the human GIP hormone with a C₂₀ fatty-diacid portion attached which, via acylation technology, can bind to albumin in order to provide a dose of the drug, by means of subcutaneous injection, once a week, which is appropriate to its a half-life of about five days. Tirzepatide, developed by Eli Lilly, was approved, under the brand name Mounjaro, by the United States Food and Drug Administration in May 2022. This started the ‘twincretin’ era of enormously important and appealing dual therapeutic options for diabetes and obesity, as well as advanced management of closely related cardiometabolic settings, which constitute the leading cause of morbidity, disability, and mortality worldwide. Herein, we present the key characteristics of tirzepatide in terms of synthesis, structure, and activity, bearing in mind its advantages and shortcomings. Furthermore, we briefly trace the evolution of this kind of medical agent and discuss the development of clinical studies.     

Critical Review on Metal-Based Cosmetic Products

Most people utilize cosmetics to enhance or improve their physical appearance, regardless of their gender, race, or age. Heavy metals (HMs) are impurities or ingredients in many cosmetic products. According to recent studies, these metals can result in a variety of skin and health issues. Numerous studies demonstrate that the mismanaged formulation of such products without sufficient standardization of toxic metals throughout the production process is the primary reason for the high level of HM contamination in the samples. In order to prevent human exposure to such dangerous HMs, it is vital to monitor and manage the fate of HMs in cosmetic items, especially unbranded ones. Due to the wasteful interest of producers in making extra profit, the standards are not being imposed. Moreover, consumers are also ready to compromise with the product due to their unawareness of its hazardous impact on their skin and bodies. Short-term results on their looks may cause fatal effects on their health. Another significant issue that requires attention is the lack of safety regulations in the country for evaluating HMs in cosmetic products. Additionally, there is an urgent need to establish acceptable limits for potential impurities in cosmetic products that must be enforced at local levels. This review provides a comprehensive insight into the content of HMs in cosmetics and their effects on several organs and the site of application.     

Water Induced Alterations in Self-Assembly of a Bio-Surfactant in Deep Eutectic Solvent for Enhanced Enzyme Activity

Deep eutectic solvents (DESs) meet important requirements for green solvent technology, including non-toxicity, biodegradability, sustainability, and affordability. Despite possessing low cohesive energy density than water, DESs have been found to support the self-assembly of amphiphiles. It is very much pertinent to examine the effect of water on self-assembly of surfactants in DESs as the presence of water alters the inherent structure of DES, which is expected to affect the characteristic properties of self-assembly. Following this, we have investigated the self-assembly of amino-acid based surfactant, Sodium N-lauroyl sarcosinate (SLS), in DES-water mixtures (10, 30 and 50 w/w% of water) and explored the catalytic activity of Cytochrome-c (Cyt-c) in the formed colloidal systems. Investigations using surface tension, fluorescence, dynamic light scattering (DLS), and isothermal titration calorimetry (ITC) have shown that DES-water mixtures promote the aggregation of SLS, resulting in the lower critical aggregation concentration (cac ∼1.5–6-fold) of the surfactant as compared to water. The nanoclustering of DES at low water content and it's complete de-structuring at high water content affects the self-assembly in a contrasting manner governed by different set of interactions. Further, Cyt-c dispersed in DES-water colloidal solutions demonstrated 5-fold higher peroxidase activity than that observed in phosphate buffer.