The invention relates to new photolabile coumarinylmethyl esters of cyclic nucleotides of general formula I
wherein
R
1
represents hydrogen, bromine or p-chlorophenylthio
R
4
represents 7-carboxymethoxy, 6,7-, 5,7- or 7,8-bis-(carboxymethoxy), 7-C
1
-C
3
-alkoxycarbonylmethoxy, 6,7-bis(C
1
-C
3
-alkoxycarbonylmethoxy), 5,7-bis(C
1
-C
3
-alkoxy-carbonylmethoxy), or 7,8-bis(C
1
-C
3
-alkoxycarbonylmethoxy),
R
2
represents —NH
2
and R
3
is hydrogen (adenine residue), or
R
2
represents —OH and R
3
represents NH
2
(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.
该发明涉及一般式I的新型光敏性
香豆素甲
酯环
核苷酸,其中R1代表
氢、
溴或对
氯苯硫基,R4代表7-羧甲
氧基、6,7-、5,7-或7,8-双(羧甲
氧基)、7-C1-C3-烷
氧羰基甲
氧基、6,7-双(C1-C3-烷
氧羰基甲
氧基)、5,7-双(C1-C3-烷
氧羰基甲
氧基)或7,8-双(C1-C3-烷
氧羰基甲
氧基),R2代表—NH2,R3为
氢(
腺嘌呤残基),或R2代表—OH,R3代表NH2(
鸟嘌呤残基)。这些创新化合物在
生物学上是不活性的,在
水性缓冲溶液中具有高溶解度,在光解离中具有高效率和快速的释放动力学,同时对溶剂解离具有高抗性。