Synthesis of propargylamine: pioneering a green path with non-conventional KA2 coupling approach.

The KA2 coupling reaction is a well-explored and versatile method for forming C-C bonds in synthetic chemistry. It is composed of ketone, amine, and alkyne, which play a major role in the synthesis of propargylamines, known for their diverse biological activities and are used in treating neurogenetical disorders. The KA2 coupling is highly challenging due to the low reactivity of ketimines toward nucleophilic attacks with metal acetylide intermediates formed by activating the C-H bond of the alkyne. Despite predominant studies conducted on thermal conditions for KA2 coupling reactions, green and sustainable approaches like non-conventional methods still have a lot to achieve. This review article provides a comprehensive introduction to the non-conventional approach in the KA2 coupling reaction, outlining its mechanisms and exploring future aspects.

Interfacial charge transfer of Carrisa edulis fruit extract capped Co3O4 nanoparticles on the surface of MK30: An efficient photocatalytic removal of methylthioninium chloride and tetracycline organic pollutants.

The in-depth usage of organic pollutants by pharmaceutical industries constitutes a major contaminant to the bodies of water due to their solubility, great mobility, ability to get attached to water bodies for a long period of time, and low biodegradability. Due to these, it may further cause disease and change the ecosystem of aqueous and other living organisms. Accordingly, effective removal of organic contaminants from waste water is a vital step in reducing the hazards. Photocatalysis is a potential technique for removing hazardous organic pollutants from wastewater. In this work, a simple ultra-sonication assisted approach, a series of Carrisa edulis fruit extract capped Co3O4 nanoparticles decorated on Montmorillonite K30 nanosheets (Co3O4/MK30) were prepared. The inherent physicochemical appearance and optical properties of as-prepared nanomaterials were investigated using a variety of analytical techniques. TEM analysis depicted the spherical shape of the Co3O4 NPs with the size of 11.25 nm. The degradation of methylthioninium chloride as a dye and tetracycline drug pollutants has been investigated in this study using individual and simultaneous photocatalysis systems in the presence of pure Co3O4 NPs and different ratios of Co3O4/MK30 nanocomposites. Owing to the generation of OH and O2 radicals, the 20% loaded Co3O4 on MK30 had the best photocatalytic performance of methylthioninium chloride (98.12%) and tetracycline degradation (87.4%), on exposing it to visible light. This research introduces a new design for MK30-based nanomaterials and proposes its use in environmental challenges.

Biological aspects of nitrogen heterocycles for amyotrophic lateral sclerosis.

Amyotrophic lateral sclerosis (ALS) is a rare, cumulative neurological deteriorating disease that disturbs the neurons (nerve cells) that control voluntary muscle movement (those muscles we choose to move). Currently, the Food and Drug Administration (FDA) approved drugs such as Radicava, Rilutek, Tiglutik, Exservan, and Nuedexta to treat ALS. Given the wide range of pharmaceutical applications of heterocyclic compounds, especially those containing the nitrogen ring systems such as pyridine, pyrimidine, and indole. These molecular frameworks have piqued the interest of medicinal chemists for further investigation in a variety of diseases. We have found several review works done on this research topic. Until now, no reviews published on the nitrogen heterocycles for treating ALS. This review examines the major causes of ALS, a brief history of medications that have been used to treat it so far, and the most recent breakthroughs in nitrogen ring systems for treating ALS. The novelty of this study provides insights on several effective synthetic techniques for nitrogen-based heterocyclic medications that operate as potent anti-inflammatory treatments and guard against ALS. KEY POINTS: • Pharmacological activity of heterocyclic compounds. • Neurodegenerative diseases and their drawbacks are discussed in detail. • Recent survey of nitrogen heterocycles in treating ALS disease are highlighted.

Biological activity of oxadiazole and thiadiazole derivatives.

The 5-membered oxadiazole and thiadiazole scaffolds are the most privileged and well-known heterocycles, being a common and essential feature of a variety of natural products and medicinal agents. These scaffolds take up the center position and are the core structural components of numerous drugs that belong to different categories. These include antimicrobial, anti-tubercular, anti-inflammatory, analgesic, antiepileptic, antiviral, and anticancer agents. In this review, we mostly talk about the isomers 1,2,4-oxadiazole and 1,3,4-thiadiazole because they have important pharmacological properties. This is partly because they are chemical and heat resistant, unlike other isomers, and they can be used as bio-isosteric replacements in drug design. We are reviewing the structural modifications of different oxadiazole and thiadiazole derivatives, more specifically, the anti-tubercular and anticancer pharmacological activities reported over the last 5 years, as we have undertaken this as a core area of research. This review article desires to do a thorough study and analysis of the recent progress made in the important biological isomers 1,2,4-oxadiazole and 1,3,4-thiadiazol. This will be a great place to start for future research. KEY POINTS: • Five-membered heterocyclic compound chemistry and biological activity recent survey. • Synthesis and pharmacological evolution of 1,2,4-oxadiazole and 1,3,4-thiadiazole are discussed in detail. • The value and significance of heterocyclic compounds in the field of drug designing are highlighted.

A review on various aspects of organic synthesis using Comins' reagent.

Recently, researchers have shown great interest in compounds such as triflate and enotriflate that are synthesized by Comins reagent. For the above-mentioned reason, we planned to review the works related to organic synthesis using Comins reagent. So this review includes a whole new investigation of the Comins reagent which is used for stereoselective conversion of α-keto ester, enolate to enol triflate of lactone and vinyl triflate to methyl ketone. Comins reagent plays an important role in regioselectivity such as transformations of ketone or dienolates into vinyl triflates and it has a major application in highly selective oxidation in an easy and environmentally friendly manner.

Augmentation of microbial fuel cell and photocatalytic polishing technique for the treatment of hazardous dimethyl phthalate containing wastewater.

In the present paper, the potentiality of integrating microbial fuel cells (MFCs) with a photocatalytic reactor to maximize the wastewater treatment efficiency with concurrent power generation was explored. Dimethyl phthalate (DMP) and acetic acid (AA) were the employed substrate and the co-substrate, respectively, using Pseudomonas aeruginosa as a biocatalyst. MFCs operated by single substrate showed the maximum power generation of 0.75-3.84 W m-3 whereas an addition of AA as the co-substrate yielded 3-12 fold higher power generation. Pseudomonas aeruginosa produced phenazine-1-carboxylic acid in DMP-fed MFC as the metabolite whereas AA along with DMP yielded pyocyanin which reduced the charge transfer resistance. Chemical oxygen demand (COD) removal efficiency in the MFCs was circa 62% after 11 days of operation. Thereafter, it further increased albeit with a drastic reduction in power generation. Subsequently, the MFC anolyte was treated in a photocatalytic reactor under visible light irradiation and catalyzed by CuO-gC3N4. The performance of photocatalytic reactor was evaluated, with COD and total organic carbon (TOC) removal efficiency of 88% and 86% after 200 min of light irradiation. The present work suggests that the MFC can be integrated with photocatalysis as a sustainable wastewater treatment method with concurrent power generation.

Facile synthesis of CuO/CdS heterostructure photocatalyst for the effective degradation of dye under visible light.

In this work, the photocatalytic property of p-type CuO was tailored by creating a heterojunction with n-type CdS. The CuO/CdS nanocomposite photocatalyst was synthesized by the ultrasound-assisted-wet-impregnation method and the physicochemical and optical properties of the catalysts were evaluated by using N2 physisorption, X-Ray Diffraction (XRD),X-Ray Photoelectron Spectroscopy (XPS), Raman spectroscopy, Transmission electron microscopy (TEM), Energy dispersive X-Ray (EDX) mapping, Field Emission Scanning Electron Microscope (FE-SEM), UV-Vis and photoluminescence spectroscopy experiments. Detailed characterization revealed the formation of a nanocomposite with a remarkable improvement in the charge carrier (electron/hole) separation. The photocatalytic degradation efficiencies of CuO and CuO/CdS were investigated for different dyes, for instance, rhodamine B (RhB), methylene blue (MLB), methyl blue (MB) and methyl orange (MO) under visible light irradiation. The obtained dye degradation efficiencies were ~93%, ~75%, ~83% and ~80%, respectively. The quantum yield for RhB degradation under visible light was 6.5 × 10-5. Reusability tests revealed that the CuO/CdS photocatalyst was recyclable up to four times. The possible mechanisms for the photocatalytic dye degradation over CuO/CdS nanocomposite were elucidated by utilizing various scavengers. Through these studies, it can be confirmed that the conduction band edges of CuO and CdS play a significant role in producing O2-. The produced O2- degraded the dye molecules in the bulk solution whereas the valence band position of CuO acted as the water oxidation site. In conclusion, the incorporation of CuO with CdS was demonstrated to be a viable strategy for the efficient photocatalytic degradation of dyes in aqueous solutions.

Chlorotrifluoroethylidenes: an efficient and convenient approach to their synthesis.

A convenient one step synthesis of chlorotrifluoroalkyl olefins starting from aldehydes was developed. The stable reagent 2-((1-chloro-2,2,2-trifluoroethyl)sulfonyl)benzothiazole was prepared from readily available benzothiazole-2-thiol and halothane. This method comprises using stable 2-((1-chloro-2,2,2-trifluoroethyl)sulfonyl)benzothiazole according to the Julia procedure and presents new opportunities for the synthesis of trifluoroalkylidene derivatives.

Screening bioactivities of Caesalpinia pulcherrima L. swartz and cytotoxicity of extract synthesized silver nanoparticles on HCT116 cell line.

The extract of Caesalpinia pulcherrima (C. pulcherrima) is one of the common herbal drugs which have a key role in treating pyretic, microbial infections, cancer and for several other traditional systems of treatment. In our present work, we demonstrate the bioactivities of extracts and cytotoxicity of synthesized silver nanoparticles on HCT116 cell line. The qualitative phytochemical tests indicated the presence of some adequately required metabolites as follows; the total phenolic content in the aqueous extract contains a higher amount of phenolic compounds (815 ±â€¯0.013 µgmg-1). The DPPH quenching activity of the aqueous extract showed an IC50 value of 18.7 µg which was equivalent to the IC50 value of ascorbic acid (15 µg) and methanolic extract (51 µg). The test extracts showed 4.6% haemolytic activity that attributes to its protective and non-toxic nature. The zone of inhibition of aqueous extract shown against the growth of E.coli was 25 mm. Further, silver nanoparticles synthesis was carried out with the extract and was characterized by X-ray diffraction, particle size analyzer, zeta potential, TEM- EDAX and UV spectroscopy. XRD analysis indicated the crystalline nature of silver nanoparticles with a face-centered cubic structure. The data obtained from the particle size analyzer demonstrated as 155.4 nm of the size of the synthesized silver nanoparticles. The values of zeta potential (-23.4 mV) revealed that the nanoparticles were extremely stable in colloidal form. SEM indicated the spherical shape of silver nanoparticles with the size range between 177.9 nm to 251.1 nm. Beside the efficient bioactivities, the synthesized C. pulcherrima silver nanoparticles showed significant cytotoxicity effect of 77.5% on a human colon cancer cell line. Therefore, along with antioxidant, antibacterial, haemolytic activity; C. pulcherrima also accomplished satisfactory cytotoxic property in anticancer mechanism as proven by this study.

CuO/C nanocomposite: Synthesis and optimization using sucrose as carbon source and its antifungal activity.

The synthesis of bioactive CuO/C nano composite using sucrose as a capping agent is achieved through simple green approach via Response Surface Methodology. The synthesis process was done in a green environment which prevents aggregation of sucrose and promotes nanoparticles formation. The innovative approach produces sucrose as a carbon source mediated copper oxide nanocomposites (CuO/C nanocomposite) with the particle size of 50 nm. Additionally, the produced CuO/C nanocomposite were characterized using microscopic techniques like SEM, TEM and spectroscopic techniques like UV-vis and X-ray diffraction. The antifungal activities of CuO/C nanocomposite were tested against Aspergillus niger and Aspergillus flavus species. At 1000 ppm of CuO/C nanocomposite, it showed 70% restraint on A. flavus and 90% hindrance on A. niger. The fungal inhibition mechanism of bioactive CuO/C nanocomposite was discussed in this research article. The particular high antifungal performance of CuO/C nanocomposite was found against Aspergillus niger while compare to Aspergillus flavus fungal strain.

UV-light intervened synthesis of imidazo fused quinazoline and its solvatochromism, antioxidant, antifungal and luminescence properties.

The photochemical preparation of benzo[4,5]imidazo[2,1-b]quinazoline was assessed under the illumination of UV wavelength (>360 nm). The compound 3,4-dihydronaphthalen-1(2H)-one 1 with 1H-benzo[d]imidazol-2-amine 2 in the existence of KOH/DMF which lead to the aromatized compound 3. The notable remark of this reaction is that the UV irradiation (312 nm) plays a vital part in the formation of compound, 3 in shorter duration (2 h) which resulted in higher yield of 96%. Compound 3 was analyzed by H1, C13 NMR, and HRMS. Solvatochromism impacts of the compound 3 was computed with different solvents (DCM < methanol< DMF < DMSO). The compound, 3 was presented to in-vitro free radical screening strategy. The standard ascorbic acid has less IC50 value - than compound 3. Further, it was subjected to in-vitro fungicidal action against two Aspergillus species (A. flavus & niger). The anti-fungal activity of compound 3 additionally demonstrated great action, when compared antifungal specialist Fluconazole.

Biosynthesis of zinc oxide nanoparticles usingMangifera indica leaves and evaluation of their antioxidant and cytotoxic properties in lung cancer (A549) cells.

Green synthesis is an eco-friendly approach to nanoparticle production, which eliminates the use of toxic chemicals, high temperatures, and costly equipment needed for traditional physical and chemical synthesis methods. This eco-friendly approach was used in the present study to biosynthesize zinc oxide nanoparticles (ZnO NPs) from Mangifera indica (mango) leaves which were then evaluated for their antioxidant activity and cytotoxic effects on lung cancer A549 cells. Synthesized ZnO nanoparticles were characterized using UV-vis spectroscopy, XRD, SEM, and EDX analyses. The XRD and SEM analyses showed 45-60 nm as the size of synthesized nanoparticles, the pure crystal form of ZnO NPs, and the shape of the NPs as nearly spherical and hexagonal quartzite. The antioxidant potential of nanoparticles was estimated using a DPPH free radical scavenging assay. The percent of viable cells was inversely proportional to the concentration of ZnO nanoparticles at 25 µg/mL concentration. The MTT assay used for cytotoxicity evaluation depicted the significant cytotoxic effect of ZnO NPs against the A549 lung cancer cell line. The drop in the proportion of viable A549 cells after exposure to ZnO NPs was comparable to the effects of the standard drug used i.e. cyclophosphamide. Antioxidant activity of NPs was increased by increasing the concentration of NPs. The present biosynthesis approach is rapid, inexpensive and eco-friendly and it yielded highly stable ZnO NPs with significant antioxidant and anticancer potential. This is the first report of M. indicia -mediated synthesis of ZnO NPs as antioxidant and, anticancer agents for the treatment of lung cancer and subsequent therapeutic applications.

Evaluation of Octyl-ß-D-Glucopyranoside (OGP) for Cytotoxic, Hemolytic, Thrombolytic, and Antibacterial Activity.

The current study indicates that octyl-ß-D-glucopyranoside (OGP) as a detergent which has the ability to make the lipid layer stiff. OGP was subjected for toxicity studies and in vitro cytotoxicty assays on cancerous HeLa and non-cancerous myoblasts H9c2 cell lines. Test against aquatic organisms were carried out in Artemia salina and LC50 values were calculated. Hemolytic activity tested for blood bio-compalibity showed hemolysis rate of 10-16%, followed by thrombolytic activity to burst the clots in blood. Also, the samples showed good lysis when compared to the standard streptokinase. Furthermore, α-amylase activity has been carried out to check the inhibition of α-amylase by the OGP. Finally, antibacterial activity has been tested against four different pathogens and their MIC values have been calculated.

Photocatalytic degradation of synthetic food dye, sunset yellow FCF (FD&C yellow no. 6) by Ailanthus excelsa Roxb. possessing antioxidant and cytotoxic activity.

The purpose of our work is to identify the bioactive compounds of bark and leaves extract from Ailanthus excelsa Roxb. and to explore its effectiveness against synthetic food dye. The presence of primary and secondary metabolites was confirmed by carrying out phytochemicals analysis. With the prior knowledge accessible on the indispensable secondary metabolites holding antioxidant and cytotoxicity activity, the quantitative screening of total phenolic and flavonoid content in methanolic and aqueous extract of bark and leaves from Ailanthus excelsa were done. Comparatively, a higher value of flavonoid (161±0.3µg/mg) and phenolic acid content (152.4±0.14µg/mg) was found in bark extract. By FTIR analysis, the characteristic peak was obtained at 1581.63 and 1598.99cm-1 confirmed the presence of functional groups associated to flavonoids and other phenolic groups respectively. In bark extract, 81% of DPPH inhibition was observed when compared to ascorbic acid (standard) 92% of free radical scavenging activity. Bark extract from Ailanthus excelsa exhibited 71% cytotoxicity against HeLa cell line (cervical cancer). In examining the toxicity level of crude extracts with red blood cells (RBC), the bark extract was showed a very less (2.8%) haemolytic activity. They also showed maximum zone of inhibition in antibacterial activity i.e. 13±0.5mm against Escherichia coli culture. At a concentration of 10mg/mL of crude extract from A. excelsa, 55% degradation of sunset yellow dye was observed. It concludes that, the compounds present in the A. excelsa, especially the bark extract showed better photocatalytic, haemolytic, antioxidant, cytotoxicity and antibacterial activity when compared to leaves extract.

Cissus quadrangularis mediated ecofriendly synthesis of copper oxide nanoparticles and its antifungal studies against Aspergillus niger, Aspergillus flavus.

Recently, non-toxic source mediated synthesis of metal and a metal oxide nanoparticle attains more attention due to key applicational responsibilities. This present report stated that the eco-friendly synthesis of copper oxide nanoparticles (CuO NPs) using Cissus quadrangularis (C. quadrangularis) plant extract. Further the eco-friendly synthesized CuO NPs were characterized using a number of analytical techniques. The observed results stated that the synthesized CuO NPs were spherical in shape with 30±2nm. Then the eco-friendly synthesized CuO NPs were subjected for anti-fungal against two strains namely Aspergillus niger (A. niger) resulted in 83% at 500ppm, 86% of inhibition at 1000ppm and Aspergillus flavus (A. flavus) resulted in 81% at 500ppm, 85% of inhibition at 1000ppm respectively. Despite the fact that compared to standard Carbendazim, eco-friendly synthesized CuO NPs exhibits better results were discussed in this manuscript.

An overview of natural renewable bio-polymer lignin towards nano and biotechnological applications.

Lignin were said to be major bio-polymer next to cellulose which is an abundant biopolymer. This type of lignin was mostly isolated from woods which were named after their physical, morphological appearances and majorly on extracting sources. Still now there are very few reports on isolation, identification of pure lignin and isolating pathways are also not well defined. Molecular weight of lignin varies from thousands to ten thousands which are not explored accurately. Even-though lignins were surrounded by these many hurdles it has various application studies which were studied and reported. Nowadays researchers focused on synthesizing lignin nanoparticles which were subjected for various application studies in day today life. This lignin contains wide range of applications in several fields like medicinal, industrial, pharmaceuticals, etc., Most of the researcher are focused on applications like anti-oxidant and microbicidal agents. So this review will comprises of outlook of bioprocessing lignin and its application focused on nanoparticles synthesis, anti-oxidant and microbicidal agents. This was the first review on renewable bio-polymer lignin with its bio-pharmaceutical and nanobiotechnological applications.

Biosynthesis and characterization of copper oxide nanoparticles and its anticancer activity on human colon cancer cell lines (HCT-116).

The eco-friendly synthesis of nanoparticles through green route from plant extracts have renowned a wide range of application in the field of modern science, due to increased drug efficacy and less toxicity in the nanosized mediated drug delivery model. In the present study, our research groups have biosynthesized the stable and cost effective copper oxide nanoparticles (CuO NPs) from the leaves of (Ormocarpum cochinchinense) O. cochinchinense. The synthesis of crystalline CuO NPs from the leaf extract of O. cochinchinense were confirmed by various analytical techniques like UV-Visible Spectroscopy (UV-Vis), Fourier-Transform Infrared Spectroscopy (FT-IR), X-Ray Diffractometer (XRD), Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM) and Selected Area Electron Diffraction (SAED) pattern. Further the synthesized CuO NPs were screened for anticancer activity on human colon cancer cell lines (HCT-116) by MTT (3-(4,5-dimethyl-2-tiazolyl)-2,5-diphenyl-2-tetrazolium bromide) assay. The obtained result inferred that the synthesized CuO NPs demonstrated high anticancer cytotoxicity on human colon cancer cell lines (HCT-116) with IC50 value of 40µgmL-1 were discussed briefly in this manuscript.

Synthesis and insecticidal activity of acridone derivatives to Aedes aegypti and Culex quinquefasciatus larvae and non-target aquatic species.

A serious Mosquito borne yellow fever is one of the grave diseases which affect the major population. Since there is no specific treatment for yellow fever, there is a necessity to develop an effective agent. The series of acridinone analogues 3 to 5 were synthesized with help of non-conventional microwave heating and confirmed by respective spectral characterization. 5c and 3b showed highest activity to kill 90% of larvae against A. aegypti and C. quinquefasciatus, respectively. Also the active products were treated to check the mortality of non-target aquatic species. Through the reports of the larvicidal bioassay, compounds 3b against C. quinquefasciatus whereas 5c against A. aegypti were found to be more active. By keeping this as a platform, further extension of the work can be done to find out a valuable drug for controlling disease vectors.

Phyllanthus emblica seed extract mediated synthesis of PdNPs against antibacterial, heamolytic and cytotoxic studies.

Ecofriendly synthesis of Palladium nanoparticles (PdNPs) were achieved using Phyllanthus emblica (P. emblica) seeds as reducing agent. Further the ecofriendly synthesized PdNPs were subjected for various analytical techniques like UV-Vis, FT-IR, XRD, Zeta potential, SEM and TEM. The results indicated that green synthesized PdNPs were spherical in shape with average particle size of 28±2nm with moderate stability. Further the synthesized PdNPs and extract were subjected for its antibacterial studies against various disease causing pathogens by agar well diffusion method. Seed extract resulted in 8.9±1.46mm against B. subtilis and PdNPs showed 9.6±1.10mm against S. aureus and synthesized PdNPs and extract were tested for hemolytic which resulted in 20% and 10% respectively. Toxicity studies were done against Artemia salina (A. salina). The LC50 value of green synthesized P. emblica capped PdNPs and the P. emblica seed extract were found to be less toxic for A. salina with a value of 1.00µg/mL and 1.25µg/mL. In addition samples were checked for in vitro cytotoxicity assays on HeLa cell lines.

Vegetable Peel Waste for the Production of ZnO Nanoparticles and its Toxicological Efficiency, Antifungal, Hemolytic, and Antibacterial Activities.

Zinc oxide (ZnO) nanoparticles (NPs) are important materials when making different products like sun screens, textiles, and paints. In the current study, the photocatalytic effect of prepared ZnO NPs from Moringa oleifera (M. oleifera) was evaluated on degradation of crystal violet (CV) dye, which is largely released from textile industries and is harmful to the environment. Preliminarily, ZnO NP formation was confirmed using a double beam ultraviolet visible (UV-Vis) spectrophotometer; further, the NP size was estimated using XRD analysis and the functional group analysis was determined using Fourier transform infrared (FT-IR) spectroscopy. The morphology of the synthesized NPs was found to be a hexagonal shape using SEM and TEM analysis and elemental screening was analyzed using EDX. ZnO NPs were shown sized 40-45 nm and spherical in shape. The degradation percentage of ZnO NPs was calculated as 94% at 70 min and the rate of the reaction -k = 0.0282. The synthesized ZnO NPs were determined for effectiveness on biological activities such as antifungal, hemolytic, and antibacterial activity. ZnO NPs showed good antifungal activity against Alternaria saloni and Sclerrotium rolfii strains. Further, we have determined the hemolytic and antibacterial activity of ZnO NPs and we got successive results in antibacterial and hemolytic activities.