| 主权项 |
1. A tricyclic nucleoside described by general Formula I:wherein:
Bx is a heterocyclic base moiety; one of T1 and T2 is hydroxyl (—OH) or a protected hydroxyl and the other of T1 and T2 is a phosphate or a reactive phosphorus group; q1 and q2 are each, independently, H, F or Cl, at least one of q3, q4 and q5 is, independently, a group described by a general formula -A1-Xh-A2-Yn, wherein
A1 is a Ck-alkyl, Ck-alkenyl or Ck-alkynyl, with k being an integer selected from the range of 0 to 20,Xh is —C(═O)—, —C(═O)O—, —C(═O)NR—, —O—, —S—, —NR—, —C(═O)R, —C(═O)OR, —C(═O)NR2—, —OR, —SR or —NR2, with each R being selected independently from H, methyl, ethyl, propyl, butyl, acetyl and 2-hydroxyethyl, and h is 0 or 1,A2 is a Ci-alkyl, Ci-alkenyl or Ci-alkynyl, with i being an integer selected from the range of 0 to 20,Y is a substituent group attached to any carbon atom on A1 and/or A2, selected from —F, —Cl, —Br, ═O, —OR, —SR, —NR2, —NR3+, NHC(═NH)NH2, —CN, —CN, —NC, —NCO, —NCS, —SCN, —COR, —CO2R, CONR2.—R, with each R being selected independently from H, methyl, ethyl, propyl, butyl, acetyl and 2-hydroxyethyl, and n is 0, 1, 2, 3, 4, 5 or 6,wherein k+i equals at least 1,the other ones of q3, q4 and q5 are, independently, H, F or Cl, one of z1 and z2 is H and the other of z1 and z2 is H, —OH, F, Cl, OCH3, OCF3, OCH2CH3, OCH2CF3, OCH2—CH═CH2, O(CH2)2—OCH3, O(CH2)2—O(CH2)2—N(CH3)2, OCH2C(═O)—N(H)CH3, OCH2C(═O)—N(H)—(CH2)2—N(CH3)2 or OCH2—N(H)—C(═NH)NH2. |
