Various adamantylated nitrogen-containing compounds are known primarily as substances exhibiting antiviral properties. Along with the well-known and sufficiently studied adamantyl-containing amines - amantadine and rimantadine, antiviral activity is manifested by representatives of such types of compounds as adamantylated azoles, amides, sulfamides, urethanes, and a number of other. In addition, adamantylated nitrogen-containing compounds are interesting as intermediates for the synthesis of other compounds with practically significant properties. Known methods for obtaining such compounds are usually bases on the adamantylation of various N-nucleophiles by 1-halogen adamantanes or 1-adamantanol, in the presence of Lewis or Brønsted acids, i.e. in conditions that ensure the generation of 1-adamantyl cation. Despite the diversity of the existing methods of adamantylation, most of them have a number of significant drawbacks, which include non-stoichiometric use of reactants (a double or triple excess of one of the reactants is often used). Some catalysts or reagents used in these reactions are aggressive or highly toxic substances, which makes such methods inconsistent with the principles of "green" chemistry. In our work, it was shown that the interaction of 1-adamantanol in the presence of 5 molar % of aluminum triflate in nitromethane medium with such N-nucleophiles as primary carboxylic or sulfonic acid amides, ethylurethane, low-basic aromatic amines and 1,2,3-benzotriazole, provides the desired N-adamantilated products with a good yields. The proposed method of adamantylation has several advantages over those previously described and can be used in the preparation of practically significant intermediates for the synthesis of biologically active adamantyl-containing compounds.

Medicinal plants are in rich source of antimicrobial agents. The present study was carried out to evaluate the antimicrobial effect plants from same species Brassica oleceracea namely, white cabbage and red cabbage The preliminary phytochemical analysis was tested by using different extract of these plants for the presence of various secondary metabolites like alkaloids, flavonoids, tannins, saponins, terpenoids, glycosides, steroids, carbohydrates and amino acids. The in vitro antimicrobial activity was screened against clinical isolates viz gram positive bacteria Staphylococcus aureus, Streptococcus pyogenes, gram negative bacteria Escherichia coli, Pseudomonas aeruginosa .Extracts were found significant inhibition against all the pathogens.

Traditionally Kajal is known as Surma or Kohl which is used as an eye liner. Designing Herbal Kajal with medicinal plants as a cosmetic product for beautification was thought of as a novel and an innovative technique.

The main advantages of these cosmetic products are more patient compliance, water resistant property, stability and of course economical to formulate.

Looking at that the present study was carried out with the aim of formulation of Herbal Kajal with the help of two medicinal plants viz. Rosa rubiginosa and Triphala and evaluate their potential for sustained ocular delivery.

Standardization of the herbs was performed based on different physiochemical parameters and revealed the values were within the prescribed limits. The Herbal kajal was evaluated on selected parameters and its anti-microbial potential was compare with comparator products.

This paper presents a QSAR study of a series of 24 dihydropyrrole-fused and phenylazo neonicotinoid derivatives, with insecticidal activity tested against Cowpea aphids (Aphis craccivora). In this regard, the conformational search ability of the OMEGA software, was employed to model neonicotinoid conformer ensembles, using molecular mechanics calculations based on the MMFF94s (the 94s variant of the Merck Molecular) force field. The minimum energy conformers were used to calculate structural descriptors, which were further related to the insecticidal activity (pLC₅₀ values), using the multiple linear regression approach. The genetic algorithm was used for variable selection and several criteria for internal and external model validation. A robust model (r² = 0.880, r²_adj = 0.855, q²_LOO = 0.827, s = 0.2098, F = 34.295) with predictive power (CCC_ext = 0.945, r²_m= 0.824) was obtained, using the QSARINS software. The developed model can be confidently used for the prediction of the insecticidal activity of new chemicals, saving a substantial amount of time and money.

An efficient and simple synthesis of substituted 2-amino-4H-chromene-3-carbonitriles was developed by the one-pot and three-component reaction of a mixture of corresponding substituted benzaldehydes, resorcinol, and malononitrile in the presence of sodium carbonate solution as a catalyst at room temperature.

In this work, BiVO₄–graphene (BVG) photocatalyst was prepared via a facile one-step hydrothermal method and was characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The photocatalytic activity of this compound was investigated by degradation of methyl orange (MO) under visible light irradiation. The photodegradation results show that the prepared BVG nanocomposite has higher photocatalytic activity compared to pure BiVO4. This compound can degrade 98% of MO under visible light irradiation. This work indicates that BiVO4 compounds are excellent compounds for pollutant degradation under visible light irradiation.

There are several methods for the synthesis of 2-(1-adamantyl)furans, including those based on 1-adamantoyl chloride and malonic ester; 5-nitrofuran-2-carboxylic acid and 1-adamantanecarboxylic acid; 1-adamantylcarbaldehyde and propargylmagnesium bromide; 1-iodoadmantane and 2-acetylfuran. However, the disadvantages of the above methods for the synthesis of 1-adamantylated furans are the multistage synthesis schemes, in some cases the use of expensive palladium catalysts and specific reaction media or the formation of a mixture of reaction products. In addition, none of the methods is not implemented on a wide range of furan substrates, which would allow us to speak about the universality of the method. Therefore, we have developed a simple method of obtaining 2-(1-adamantyl)furans using a smaller amount of catalyst, providing a higher yield of the target products, as well as the possibility of varying the substituents in the furan ring. The result is achieved by the adamantylation of furans with 1-adamantanol in a nitromethane medium in the presence of a Lewis acid, for which aluminum or bismuth triflate was used in an amount of 10 mol%. Depending on the nature of the substituent in the furan ring, the reaction is carried out at room temperature or heated at 50-80 ° C. The method is applicable to a number of alkyl-, arylfurans, as well as to furans containing functional groups, such as carbethoxy, β-nitrovinyl, which are most promising for use in the synthesis of biologically active substances.

An expeditious, efficient and high yield conversion of ketone group in GBB adducts was obtained by the reaction with 3-formyl chromone, 2-amino pyridine and isocyanide to corresponding thio analogues is described utilizing Lawesson’s reagent. The reaction was involved microwave irradiation for both GBBR and the functional group transformation from ketone to thio ketone using Lawesson’s reagent in a one-pot fashion. The thio heterocyclic analogs of GBB products were characterized by using IR, NMR, and HRMS.

Nowadays, the treatment of Alzheimer’s disease (AD) is focused on targeting neurotransmitter functions by using acetylcholinesterase inhibitors (AChEIs) and N-methyl-D-aspartic acid (NMDA) glutamate receptor antagonists. Four of the five drugs that have been approved by the U.S. Food and Drug Administration (FDA) for AD, including tacrine and donepezil, are AChEIs. This fact together with the results of studies performed in the last decades highlighting the role of AChE enzyme and cholinergic system on Aβ plaques deposition and modulation of regional brain blood flow, respectively, have contributed to the growing interest in AChEIs. [1]

New drugs should not only be able to inhibit the enzyme but also show optimal parameters of solubility and permeability across cellular membranes, since they affect bioavailability. Considering the good properties of ionic liquids (ILs) and the potential advantages of transforming active pharmaceutical ingredients APIs into ILs, a new series of API-ILs based on two AChEIs, tacrine, a commercially available drug, and compound 1, [2] a donepezil analogue, was proposed. The design, synthesis and evaluation of the water solubility of five new API-ILs, four of them derived from tacrine and one of the donepezil analogue 1, were successfully carried out in this work.

[1] a) G. V. De Ferrari, M. A. Canales, I. Shin, L. Weiner, I. Silman and N. C. Inestrosa, Biochemistry 2001, 40, 10447-10457; b) R. M. lane, M. Kivipelto and N. H. Greig, Clin. Neuropharmacol. 2004, 27,141-149.

[2] N. Vila, P. Besada, D. Viña, M. Sturlese, S. Moro and C. Terán, RSC Adv. 2016, 6, 46170-46185

Recently there is a growing interest in covalent protease inhibitors in industry and academia caused by their longer residence times, their higher potency and their high ligand efficiency. Covalently reactive moieties which interact with activated amino acid residues such as serine or cysteine in enzymes like proteases or esterases rarely act through nucleophilic aromatic substitution (SNAr). In our previous work, we presented design and properties of electrophilic "warheads", which contain aromatic(heteroaromaric) or quinoid fragments. Some of them show high inhibition constants for cathepsin L, cathepsin B, rhodesain or dengue-protease and depending on the exact nature of the electrophile, they exhibit reversible covalent or irreversible inhibition modes. In the present work, we demonstrate the synthesis of fluorescent "warhead" candidates based on 2,1,3-benzoxadiazoles and the investigation of their physicochemical and photophysical properties. These molecules shall serve as probes for the detailed analysis of association/dissociation and of the kinetic parameters of the bond forming event.