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Heteroatoms constitute a very common fragment of a number of active pharmaceutical ingredients as well as excipients; from the point of view of significance, it is all the same if these are isosterically/bioisosterically replaced carbons/carbon substructures in aliphatic structures or real heterocycles [...]

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Abstract:In this study, a series of twenty-two ring-substituted 3-hydroxy-Nphenylnaphthalene-2-carboxanilides were prepared and characterized. The compounds were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four Staphylococcus strains and against two mycobacterial species. 3-Hydroxy-N-(2-methoxyphenyl)naphthalene-2-carboxamide showed OPEN ACCESSMolecules 2013, 18 7978 high biological activity (MIC = 55.0 µmol/L) against S. aureus as well as methicillinresistant strains. N-(2-Fluorophenyl)-3-hydroxynaphthalene-2-carboxamide showed higher activity (MIC = 28.4 µmol/L) against M. marinum than the standard isoniazid and 3-hydroxy-N-(4-nitrophenyl)naphthalene-2-carboxamide expressed higher activity (MIC = 13.0 µmol/L) against M. kansasii than the standard isoniazid. Cytotoxicity assay of effective antimicrobial compounds was performed using the human monocytic leukemia THP-1 cell line. The PET-inhibiting activity expressed by IC 50 value of the most active compound 3-hydroxy-N-(3-nitrophenyl)naphthalene-2-carboxamide was 16.9 μmol/L. The structure-activity relationships of all compounds are discussed.

Abstract:In this study, a series of twenty-two ring-substituted 2-hydroxynaphthalene-1-carboxanilides were prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Staphylococcus aureus, three methicillin-resistant S. aureus strains, Mycobacterium marinum, M. kasasii, M. smegmatis. and M. avium paratuberculosis. The compounds were also tested for their activity related OPEN ACCESSMolecules 2013, 18 9398 to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. 2-Hydroxy-N-phenylnaphthalene-1-carboxanilide and 2-hydroxy-N-(3-trifluoromethylphenyl)naphthalene-1-carboxamide (IC 50 = 29 µmol/L) were the most active PET inhibitors. Some of tested compounds showed the antibacterial and antimycobacterial activity against the tested strains comparable or higher than the standards ampicillin or isoniazid. Thus, for example, 2-hydroxy-N-(3-nitrophenyl)naphthalene-1-carboxamide showed MIC = 26.0 µmol/L against methicillin-resistant S. aureus and MIC = 51.9 µmol/L against M. marinum, or 2-hydroxy-N-phenylnaphthalene-1-carboxamide demonstrated MIC = 15.2 µmol/L against M. kansasii. The structure-activity relationships for all compounds are discussed.

The lack of the wide spectrum of biological data is an important obstacle preventing the efficient molecular design. Quinoline derivatives are known to exhibit a variety of biological effects. In the current publication, we tested a series of novel quinoline analogues for their photosynthesis-inhibiting activity (the inhibition of photosynthetic electron transport in spinach chloroplasts (Spinacia oleracea L.) and the reduction of chlorophyll content in Chlorella vulgaris Beij.). Moreover, antiproliferative activity was measured using SK-N-MC neuroepithelioma cell line. We described the structure-activity relationships (SAR) between the chemical structure and biological effects of the synthesized compounds. We also measured the lipophilicity of the novel compounds by means of the RP-HPLC and illustrate the relationships between the RP-HPLC retention parameter logK (the logarithm of capacity factor K) and logP data calculated by available programs.

The series of quinaldine derivatives were prepared, some of them by means of novel synthetic methods. The synthetic approach, analytical and spectroscopic data of all newly synthesized compounds are presented. The prepared compounds were tested for their in vitro antifungal activity as well as for their photosynthesis-inhibiting activity (the inhibition of photosynthetic electron transport in spinach chloroplasts (Spinacia oleracea L.) and the reduction of chlorophyll content in Chlorella vulgaris Beij.). Structure-activity relationships among the chemical structure, the physical properties and the biological activities of the evaluated compounds are discussed in the article.

Dietary supplements and foods for special medical purposes are special medical products classified according to the legal basis. They are regulated, for example, by the European Food Safety Authority and the U.S. Food and Drug Administration, as well as by various national regulations issued most frequently by the Ministry of Health and/or the Ministry of Agriculture of particular countries around the world. They constitute a concentrated source of vitamins, minerals, polyunsaturated fatty acids and antioxidants or other compounds with a nutritional or physiological effect contained in the food/feed, alone or in combination, intended for direct consumption in small measured amounts. As nanotechnology provides “a new dimension” accompanied with new or modified properties conferred to many current materials, it is widely used for the production of a new generation of drug formulations, and it is also used in the food industry and even in various types of nutritional supplements. These nanoformulations of supplements are being prepared especially with the purpose to improve bioavailability, protect active ingredients against degradation, or reduce side effects. This contribution comprehensively summarizes the current state of the research focused on nanoformulated human and veterinary dietary supplements, nutraceuticals, and functional foods for special medical purposes, their particular applications in various food products and drinks as well as the most important related guidelines, regulations and directives.