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ASPARTYL DERIVATIVES OF HISTAMINE, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND THEIR USING AS MODULATORS OF ENZYME ACTIVITY OF ANTIOXIDANT PROTECTION
ASPARTYL DERIVATIVES OF HISTAMINE, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND THEIR USING AS MODULATORS OF ENZYME ACTIVITY OF ANTIOXIDANT PROTECTION
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机译：组氨酸的天冬氨酰衍生物，其制备方法，药物组成及其作为抗氧化剂保护酶活性的调节剂
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FIELD: bioorganic chemistry, biochemistry, pharmacy.;SUBSTANCE: invention relates to novel aspartyl derivatives of histamine of the general formula (I): , wherein R means hydrogen atom (H), or , or that are able to modulate activity of enzymes of antioxidant protection - superoxide dismutase (SOD) and catalase. Also, invention relates to using the known compounds of the general formula (I) for the same designation wherein at the same values of X the value R represents acetyl group, and to their pharmaceutically acceptable salts. Also, invention relates to a pharmaceutical composition possessing capacity to modulate activity of SOD and catalase and comprising the effective amount of compound of the general formula (I), and to a method for synthesis of compounds of the general formula (I). Method involves interaction of pentafluorophenyl ester N-Z-, - or -benzyl ester of aspartic acid with histamine followed by hydrogenolysis without isolation of intermediated protected derivatives of aspartyl histamine.;EFFECT: improved method of synthesis, valuable biochemical properties of derivatives.;12 cl, 3 tbl, 2 sch, 2 dwg, 8 ex
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机译：技术领域：本发明涉及具有通式（I）的组胺的新型天冬氨酰衍生物：<图像文件=“ 00000006.GIF” he =“ 14” id =“ imag00000006” imgContent =“未定义” imgFormat =“ GIF” wi =“ 75” />，其中R表示氢原子（H），<图像文件=“ 00000007.GIF” he =“ 14” id =“ imag00000007” imgContent =“未定义” imgFormat = “ GIF” wi =“ 49” />或<图像文件=“ 00000008.GIF” he =“ 17” id =“ imag00000008” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 43” />或<图片文件=“ 00000009.GIF” he =“ 17” id =“ imag00000009” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 22” />能够调节抗氧化保护酶-超氧化物歧化酶（ SOD）和过氧化氢酶。同样，本发明涉及将已知的通式（I）的化合物用于相同的名称，其中在相同的X值处，R值代表乙酰基，及其药学上可接受的盐。此外，本发明涉及具有调节SOD和过氧化氢酶活性并且包含有效量的通式（I）的化合物的药物组合物，并且涉及合成通式（I）的化合物的方法。该方法涉及天冬氨酸的五氟苯基酯N -Z-，-或-苄基酯与组胺的相互作用，然后进行氢解而无需分离中间体保护的天冬氨酰组胺衍生物。效果：改进的合成方法，有价值的生化特性衍生物。; 12 cl，3 tbl，2 sch，2 dwg，8 ex
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