| 主权项 |
1. A compound of Formula I: wherein:
R is O—R1 or NR4R1′;R′ is N(R4)C(R2a)(R2b)C(═O)OR3 or —OR3;
R1′is —C(R2a)(R2b)C(═O)OR3;R1 is H, 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, —COR1b, —SO2(R1c), —NHSO2(R1c), nitro or cyano;
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 are independently H, lower alkyl, —(CH2)rN(R1a)2, lower hydroxyalkyl, —CH2SH, —(CH2)S(O)pMe, —(CH2)3NHC(═NH)NH2, (1H-indol-3-yl)methyl, (1H-indol-4-yl)methyl, —(CH2)mC(═O)R1b, aryl and aryl lower alkyl, wherein aryl may optionally be substituted with one or more hydroxy, lower alkyl, lower alkoxy, halo, nitro or cyano; m is 0 to 3; p is 0 to 2; r is 1 to 6;or R2a is H and R2b and R4 together form (CH2)n; n is 4 or 5;R3 is H, lower alkyl, lower haloalkyl, phenyl or phenyl lower alkyl;R4 is H, lower alkyl, or R2b and R4 together form (CH2)3;R5 is H, C(═O)R1c, C(═O)R1b, P(═O)(OR1)(OR1a), or P(═O)(OR1)(NR4R7);Base is uracil, cytosine, guanine, adenine, thymine, 7-deaza-7-fluoro adenosine or heterocycloalkyl, each of which may optionally substituted with one or more hydroxy, lower alkyl, lower alkoxy, halo, nitro or cyano; andX is O or S;or a pharmacologically acceptable salt thereof. |
