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• W1752912102 abstract "It is well known that benzoxazole derivatives have a wide range of biological activities. Recently, it was shown that the derivatives of benzoxazoltione, substituted at an amino group inhibit photosynthesis in chloroplasts and algae such as Chlorela vulgaris. It was observed that the inhibitory effect decreases with increasing lipophilicity of substances in the series. The lipophilicity or hydrophilicity are expressed by the partition coefficient, which is a very important factor that characterize the pharmacokinetic profile of a chemical compound. We studied the structural descriptors that contribute to the biological activity of substances. For a series of nine substances, results show that descriptors CSAA, CSEV and TFES appear to be responsible for the inhibitory activity of these substances. INTRODUCTION Lately intensified research regardig those chemicals capable of destroying vegetable pests of crops by inhibiting photosynthesis of the second system of these pests (PS I) /1-3/. It is known that in the photosynthesis drives of chloroplasts which are, particularly there tilakoide membranes, photosynthesis reactions take place with the illuminating radiation. The light energy is collected by the chloroplast pigments antenna and transferred to reaction centers. For photosynthesis to be effective, light is distributed evenly between the two systems of photosynthesis so that they derive with the same speed. Plants do this using the redox state of the quinone tank which regulates the distribution of light energy between the two systems of photosynthesis (Figure 1). Figure 1. The process of photosynthesis /2/ If the quinone tank is too low, the first system of photosynthesis (PS I), ie the direct one, operates too slowly, requiring more light energy. n CO2 + n H2O → (CH2O)n + n O2 Analele Universitaţii din Craiova, seria Agricultura – Montanologie – Cadastru (Annals of the University of Craiova Agriculture, Montanology, Cadastre Series) Vol. XLIV 2014 15 This is done by activating an enzyme, called kinases, which stimulates the phosphorylation reaction LHCP (Light Harvesting Complex Protein) which direct the light energy to the first system of photosynthesis. If the quinone tank is oxidized, the kinase is inactivated, and LHCP is dephosphorylated by an enzyme called phosphatase. In the latter case, much of the light energy is directed to the photosynthetic system PS II, which is called the dark reaction system. Thus light energy is converted by the two photochemical reactions systems into chemical energy by redox reactions. Some chemicals affect the electron transport system, acting as a oxidant terminal for the first system of photosynthesis, stimulating beyond measure electronic transport. Other substances compete and blocks access of plastoquinone to the binding site QB of the protein D1 in the second system of photosynthesis. In this way it inhibited the reduction of plastochinonei through photosynthesis. As a result, the electronic properties and mediation of a proton, in the D1 proteincase, are strongly influenced by the presence of fluids inside the chloroplast of such substances and their concentration in the fluid. MATERIALS AND METHODS In this context, it is well known that benzoxazoltiona derivatives have a wide range of biological activities /4-6/ namely, it was found that 3-(2-Aminomethyl-benzothiazol-6 alkylsulfanyl)-2-benzoxazoltiones inhibits photosynthesis in chloroplasts /4/. The biological activity of these derivatives depends, as expected, of the partition coefficient and, therefore, the lipophilicity or hydrophilicity of these substances. This coefficient is a physicochemical factor directly influencing the pharmacokinetics profile of a chemical and, indirectly, its pharmacodynamic profile. The partition coefficient:" @default.
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• W1752912102 date "2014-01-01" @default.
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• W1752912102 title "The study of partition coefficient octanol/water for 3-(2-alchylsulfanyl-6-benzothiazolylaminomethyl)-2-benzoxazoltione as photosynthesis inhibitors." @default.
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