Hampton A, Sasaki T, Perini F, Slotin L A, Kappler F
J Med Chem. 1976 Aug;19(8):1029-33. doi: 10.1021/jm00230a011.
Derivatives of adenosine 5'-phosphate (AMP) have been synthesized in which the phosphoester (POCH2) grouping of AMP is replaced by PCH(R)CH2 where R is OC(O)Me, CH2NHCOMe, CH2NHCOEt, and CH2NHCOOR' (R' = Me, Et, and Pr). The 2',3'-O-isopropylidene and 2', 3'-di-O-acetyl derivatives of AMP were also prepared. All compounds were competitive inhibitors of rabbit muscle AMP aminohydrolase with enzyme-inhibitor dissociation constants (Ki values) of 330, 20, 17, 19, 16, 14, 260, and 105 muM, respectively. All compounds were substrates except those in which R was CH2NHCOEt and CH2NHCOOR' (R'=Me, Et, and Pr). The previously described allo and talo epimers of 5'-C-acetylaminomethyl-AMP and the allo epimer of 5'-C-propionylaminomethyl-AMP were substrates and competitive inhibitors with Ki values of 18, 47, and 42 muM, respectively. The talo epimer of 5'-C-propionylaminomethyl-AMP was not a substrate and was a noncompetitive inhibitor, Ki
已经合成了5'-磷酸腺苷（AMP）的衍生物，其中AMP的磷酸酯（POCH2）基团被PCH(R)CH2取代，其中R为OC(O)Me、CH2NHCOMe、CH2NHCOEt和CH2NHCOOR'（R' = Me、Et和Pr）。还制备了AMP的2',3'-O-异丙叉基和2',3'-二-O-乙酰基衍生物。所有化合物都是兔肌肉AMP氨基水解酶的竞争性抑制剂，酶-抑制剂解离常数（Ki值）分别为330、20、17、19、16、14、260和105μM。除了R为CH2NHCOEt和CH2NHCOOR'（R' = Me、Et和Pr）的那些化合物外，所有化合物都是底物。先前描述的5'-C-乙酰氨基甲基-AMP的别和塔罗差向异构体以及5'-C-丙酰氨基甲基-AMP的别差向异构体是底物和竞争性抑制剂，Ki值分别为18、47和42μM。5'-C-丙酰氨基甲基-AMP的塔罗差向异构体不是底物，是一种非竞争性抑制剂，Ki
