The growing interest in plant-derived compounds and synthesis of metallopolymer nanocomposites (MPNCs) especially silver chitosan nanocomposites (AgCS-NCs) emerges as a useful platform to encapsulate and deliver plant-based anticancer drugs. This work presents the synthesis of AgCS-NCs by using Moringa oleifera aqueous leaf extract (MOAE) and the effect of concentration of MOAE on physicochemical properties of AgCS-NCs followed by its anticancer effect on MCF-7 cell line. The results of UV-visible spectroscopy (UV-Vis) and Scanning electron microscopy (SEM) showed successful formation of AgCS-NCs.
View Article and Find Full Text PDFEssential oils (EOs) are gaining popularity due to their potent antibacterial properties, as well as their applications in food preservation and flavor enhancement, offering growth opportunities for the food industry. However, their widespread use as food preservatives is limited by authenticity challenges, primarily stemming from adulteration with cheaper oils. This study investigated a rapid, cost-effective, and non-destructive method for assessing the authenticity of widely used Mentha and Ocimum EOs.
View Article and Find Full Text PDF2,3-Dihydrobenzofurans are noteworthy scaffolds in organic and medicinal chemistry, constituting the structural framework of many of the varied medicinally active organic compounds. Moreover, a diverse variety of biologically potent natural products also contain this heterocyclic nucleus. Reflecting on the wide biological substantiality of dihydrobenzofurans, several innovative and facile synthetic developments are evolving to achieve these heterocycles.
View Article and Find Full Text PDFA novel series of substituted benzofuran-tethered triazolylcarbazoles was synthesized in good to high yields (65-89%) via -alkylation of benzofuran-based triazoles with 2-bromo--(9-ethyl-9-carbazol-3-yl)acetamide. The inhibitory potency of the synthesized compounds against SARS-CoV-2 was evaluated by enacting molecular docking against its three pivotal proteins, namely, M (main protease; PDB ID: 6LU7), the spike glycoprotein (PDB ID: 6WPT), and RdRp (RNA-dependent RNA polymerase; PDB ID: 6M71). The docking results indicated strong binding affinities between SARS-CoV-2 proteins and the synthesized compounds, which were thereby expected to obstruct the function of SARS proteins.
View Article and Find Full Text PDFThe Barbier reaction is significantly referred to as one of the efficient carbon-carbon bond forming reactions which involves the treatment of haloalkanes and carbonyl compounds by utilizing the catalytic role of a diverse range of metals and metalloids. The Barbier reaction is tolerant to a variety of functional groups, allowing a broad substrate scope with the employment of lanthanides, transition metals, amphoteric elements or alkaline earth metals. This reaction is also water-resistant, thereby overcoming the challenges posed by moisture sensitive organometallic species involving C-C bond formation reactions.
View Article and Find Full Text PDFObjective: Behaviour Change Communication (BCC) intervention programmes often lack documentation of successful processes. This manuscript aims to describe the development of Program Impact Pathway (PIP) using Theory of Change (ToC) approach for a mHealth BCC intervention titled 'Mobile Solutions Aiding Knowledge for Health Improvement (M-SAKHI)' aimed at reducing stunting in infants at 18 months of age.
Design: The PIP was developed using ToC to design the intervention and plan its implementation.
Benzofurans have intrigued both pharmaceutical researchers and chemists owing to the medicinal usage of their derivatives against copious disease-causing agents (i.e., bacteria, viruses, and tumors).
View Article and Find Full Text PDFIn this study, a series of 1,2,4-triazole-tethered β-hydroxy sulfide scaffolds 11a-h was synthesized in good to remarkable yields (69-90%) through the thiolysis of oxiranes by the thiols in aqueous basic catalytic conditions. The synthesized 1,2,4-triazole-tethered β-hydroxy sulfides were screened against bacterial tyrosinase enzyme, and Gram-positive and Gram-negative bacterial cultures , () & () . Among the synthesized derivatives, the molecules 11a (IC = 7.
View Article and Find Full Text PDFMyasthenia gravis (MG) is an autoimmune disorder characterized by fluctuating weakness and fatigue in ocular, bulbar, limb, or respiratory muscles. Initially, more than half of MG patients experience isolated ocular symptoms, such as ptosis, diplopia, or muscle paresis. This case report presents a unique occurrence of MG in a four-year-old female, showcasing a two-year history of sudden onset, persistent yet fluctuating unilateral ptosis accompanied by exo-deviation and adduction deficit in the right eye.
View Article and Find Full Text PDFOral squamous cell carcinoma (OSCC) is the most prevalent cancer in Pakistani population because of consumption of different tobacco-containing products whether smoked or chewed. These patients commonly report at a late stage of the disease. The patient's survival only depends upon early-stage diagnosis.
View Article and Find Full Text PDFTriazoles, nitrogen-containing heterocycles, have gained attention for their applications in medicinal chemistry, drug discovery, agrochemicals, and material sciences. In the current study, we synthesized novel derivatives of N-substituted 2-((5-(3-bromophenyl)-4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-phenylpropanamide and conducted a comprehensive investigation using density functional theory (DFT). These novel structural hybrids of 1,2,4-triazole were synthesized through the multi-step chemical modifications of 3-bromobenzoic acid (1).
View Article and Find Full Text PDFBenzofuran, 1,3,4-oxadiazole, and 1,2,4-triazole are privileged heterocyclic moieties that display the most promising and wide spectrum of biological activities against a wide variety of diseases. In the current study, benzofuran-1,3,4-oxadiazole - and benzofuran-1,2,4-triazole compounds - were tested against HCV NS5B RNA-dependent RNA polymerase (RdRp) utilizing structure-based screening via a computer-aided drug design (CADD) approach. A molecular docking approach was applied to evaluate the binding potential of benzofuran-appended 1,3,4-oxadiazole and 1,2,4-triazole - molecules.
View Article and Find Full Text PDFPiperazine is a privileged moiety that is a structural part of many clinical drugs. Piperazine-based scaffolds have attracted the attention of pharmaceutical and medicinal scientists to develop novel, efficient therapeutic agents owing to their significant and promising biological profile. In the current study, an ecofriendly ultrasonic-assisted synthetic approach was applied to achieve a novel series of 1-tosyl piperazine dithiocarbamate acetamide hybrids - which was evaluated for in vitro tyrosinase inhibition and thrombolytic and hemolytic cytotoxic activities.
View Article and Find Full Text PDFHerbal medicines are popular natural medicines that have been used for decades. The use of alternative medicines continues to expand rapidly across the world. The World Health Organization suggests that quality assessment of natural medicines is essential for any therapeutic or health care applications, as their therapeutic potential varies between different geographic origins, plant species, and varieties.
View Article and Find Full Text PDFSimmons-Smith cyclopropanation is a widely used reaction in organic synthesis for stereospecific conversion of alkenes into cyclopropane. The utility of this reaction can be realized by the fact that the cyclopropane motif is a privileged synthetic intermediate and a core structural unit of many biologically active natural compounds such as terpenoids, alkaloids, nucleosides, amino acids, fatty acids, polyketides and drugs. The modified form of Simmons-Smith cyclopropanation involves the employment of EtZn and CHI (Furukawa reagent) toward the total synthesis of a variety of structurally complex natural products that possess broad range of biological activities including anticancer, antimicrobial and antiviral activities.
View Article and Find Full Text PDFTriazole-based acetamides serve as important scaffolds for various pharmacologically active drugs. In the present work, structural hybrids of 1,2,4-triazole and acetamides were furnished by chemically modifying 2-(4-isobutylphenyl) propanoic acid (). Target compounds were produced in considerable yields (70-76%) by coupling the triazole of compound 1 with different electrophiles under different reaction conditions.
View Article and Find Full Text PDFRing expansion reactions fascinate synthetic chemists owing to their importance in synthesizing biologically active compounds and their efficacy in medicinal chemistry. The present review summarizes a number of synthetic methodologies, including stereoselective and regioselective pathways adopted by scientists, for framing medium- to large-size carbo- and heterocycles involving lactams, lactone, azepine and azulene derivatives via ring expansion of six-membered carbo- and heterocycles that have been reported from 2007-2022. Numerous rearrangement and cycloaddition reactions involving Tiffeneau-Demjanov rearrangement, Aza-Claisen rearrangement, Schmidt rearrangement, Beckmann rearrangement, etc.
View Article and Find Full Text PDFIn this study, we have investigated ciprofloxacin-based acetanilides for their in-vitro inhibitory study against gram +ve, -ve bacteria and serine protease activity. The compounds 4e and 4g showed excellent antibacterial activity against Bacillus subtilis with a zone of inhibition (ZI) values of 40 ± 0.9 mm, 37 ± 1.
View Article and Find Full Text PDFIdentification of plant species is a crucial process in natural products. , often referred to as the queen of herbs, is one of the most versatile and globally used medicinal herbs for various health benefits due to it having a wide variety of pharmacological activities. Despite there being significant global demand for this medicinal herb, rapid and comprehensive metabolomic fingerprinting approaches for species- and variety-specific classification are limited.
View Article and Find Full Text PDFThe development of an economical method for the synthesis of biologically active compounds was the major goal of this research. In the present study, we have reported the ultrasound-radiation-assisted synthesis of a series of novel N-substituted 1,2,4-triazole-2-thiol derivatives. The target compounds 6a−f were efficiently synthesized in significant yields (75−89%) by coupling 1,2,4-triazole of 2-(4-isobutylphenyl) propanoic acid 1 with different electrophiles using ultrasound radiation under different temperatures.
View Article and Find Full Text PDFThe antileishmanial activity of a series of ()-2-(heteroarylmethylene)-3(2)-benzofuranone derivatives, possessing 5-nitroimidazole or 4-nitroimidazole moieties, was investigated against Leishmania major promastigotes and some analogues exhibited prominent activities. Compounds with IC values lower than 20 μM were further examined against L. donovani axenic amastigotes.
View Article and Find Full Text PDFACS Appl Mater Interfaces
August 2022
Persistent organic pollutants (POPs) have become a major global concern due to their large amount of utilization every year and their calcitrant nature. Due to their continuous utilization and calcitrant nature, it has led to several environmental hazards. The conventional approaches are expensive, less efficient, laborious, time-consuming, and expensive.
View Article and Find Full Text PDFIncense burning is practiced alongside many sacred rituals across different regions of the world. Invariable constituents of incense brands are 21% (by weight) herbal and wood powder, 33% bamboo stick, 35% fragrance material, and 11% adhesive powder. Major incense-combustion outputs include particulate matter (PM), volatile organic content, and polyaromatic hydrocarbons.
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