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photolabile cumarinylmethylester of cyclic nucleotides, methods for their production and their use

机译:环状核苷酸的光不稳定性豆香油基甲基酯,其生产方法和用途

摘要

The invention relates to new photolabile coumarinylmethyl esters of cyclic nucleotides of general formula I wherein RSUP1 /SUPrepresents hydrogen, bromine or p-chlorophenylthio RSUP4 /SUPrepresents 7-carboxymethoxy, 6,7-, 5,7- or 7,8-bis-(carboxymethoxy), 7-CSUB1/SUB-CSUB3/SUB-alkoxycarbonylmethoxy, 6,7-bis(CSUB1/SUB-CSUB3/SUB-alkoxycarbonylmethoxy), 5,7-bis(CSUB1/SUB-CSUB3/SUB-alkoxy-carbonylmethoxy), or 7,8-bis(CSUB1/SUB-CSUB3/SUB-alkoxycarbonylmethoxy), RSUP2 /SUPrepresents -NHSUB2 /SUBand RSUP3 /SUPis hydrogen (adenine residue), or RSUP2 /SUPrepresents -OH and RSUP3 /SUPrepresents NHSUB2 /SUB(guanine residue) The inventive compounds are biologically inactive and exhibit high solubility in aqueous buffer solutions, high efficiency in photocleavage and rapid kinetics of liberation, together with high resistance to solvolysis.
机译:本发明涉及通式I的环状核苷酸的新的光不稳定香豆基甲基酯,其中R 1 代表氢,溴或对氯苯硫基R 4 代表7-羧基甲氧基6,7 -,5,7-或7,8-双-(羧基甲氧基),7-C 1 -C 3 -烷氧基羰基甲氧基,6,7-双(C 1 -C 3 -烷氧基羰基甲氧基),5,7-双(C 1 -C 3 -烷氧基羰基甲氧基)或7,8-bis(C 1 -C 3 -烷氧基羰基甲氧基),R 2 代表-NH 2 并且R 3 是氢(腺嘌呤残基),或R 2 代表-OH,R 3 代表NH 2 (鸟嘌呤残基)本发明的化合物是生物惰性的,并且在缓冲水溶液中显示出高溶解度,在光裂解中具有高效率,并且具有快速的释放动力学,以及对溶剂分解的高抗性。

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