| 主权项 |
1. A compound of formula I. wherein: Y is H or P(═X)(R)(R′);
R is O—R1 or NHC(R2a)(R2b)C(═O)OR3;R′ is N(R4)C(R2a)(R2b)C(═O)OR3, —OP(═O)(OH)OP(═O)(OH)OH, or —OR3;
R1 is H, lower alkyl, lower haloalkyl, or aryl, wherein aryl is phenyl or naphthyl, optionally substituted with one or more lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halo, lower haloalkyl, —N(R1a)2, acylamino, —SO2N(R1a)2, —C(═O)R1b, —SO2R1c, —NHSO2R1c, nitro, cyano, or R1″;
each R1a is independently H or lower alkyl;each R1b is independently —OR1a or —N(R1a)2;each R1c is lower alkyl;each R2a and R2b is independently H, lower alkyl, —(CH2)rN(R1a)2, lower hydroxyalkyl, —CH2SH, —(CH2)S(O)pMe, —(CH2)nNHC(═NH)NH2, (1H-indol-3-yl)Me, (1H-indol-4-yl)Me, —(CH2)mC(═O)R1b, aryl or aryl lower alkyl, wherein aryl and aryl lower alkyl are optionally substituted with one or more hydroxy, lower alkyl, lower alkoxy, halo, nitro or cyano; m is 0, 1, or 2; n is 1, 2, or 3; p is 1 or 2; r is 1 or 2;or R2a is H and R2b and R4 together form (CH2)n;each R3 is independently H, lower alkyl, lower haloalkyl, phenyl or phenyl lower alkyl, wherein phenyl and phenyl lower alkyl are optionally substituted with lower alkoxy;or R3 and R1″ together form CH2;each R4 is independently H, lower alkyl;or R2b and R4 together form (CH2)3; each of Rw, Rx, and Ry is independently H, OH, or F; Rz is H or OH; or R3 and Rx together form a bond; or R1 and Rx together form a bond; X is O or S; and Base is uracil, cytosine, guanine, adenine, thymine, or heterocycloalkyl, each of which may optionally be substituted with one or more hydroxy, lower alkyl, lower alkoxy, halo, nitro or cyano; or a pharmacologically acceptable salt thereof. |
