| 摘要 |
A purine L-nucleoside derivative has the formula I wherein: R1 R2, R3, R4, R5, R2' and R3' are independently H, F, Cl, Br, I, N3, -CN, -OR', -NR'2, -SR', -NHNH2, -NHOH, CHO, COOR', CONR'2 or optionally substituted alkyl, alkenyl, alkynyl, aryl, or aralkyl; W = O, S, CH2 or Se; Z1, Z2 are independently N, C or CH; Z3, Z4, Z5 are independently -NR-, -O-, -S-, -Se-, C=O, -C=S, -S=O, -CR=CR-, -CR=N- or -N=N-; R is H, F, Cl, Br, I, N3, -CN, -OR', -NR'2, -SR', -NHNH2, -NHOH, -NO2, CHO, COOR', CONH2, -C(O)-NH2, -C(S)-NH2, -C(NH)-NH2, -C(NOH)-NH2 or substituted alkyl, alkenyl, alkynyl, aryl or aralkyl, the chemical bond between Z3 and Z4 or Z4 and Z5 is C-C, C=C, C-N, C=N, N-N, N=N, C-S or N-S; X and Y are independently H, F, Cl, Br, I, N3, -S-NH2, -S(O)-NH2, -S(O)2-NH2, -CN, -COOR', -CONR'2, -OR', -NR'2, -SR', NHNH2, -NHOH or optionally substituted alkyl, alkenyl, alkynyl, aryl, or aralkyl provided that i) when W is O, R1 and R4 are H, R2, R3 and R5 is OH then Z1, Z2 and Z5 is not N, Z2 is not S, Z4 is not CO, Y is not NH2 and X is not OH; ii) when R2 and R3 are OH then X is not NH2; iii) when X is halo, NH2, H, OH or SH and /or Y is halo, NH2, H, OH or SH, then R2 and/or R3 are not H; iv) when Y is NH2 then Z3 is not O or S and v) when W is S at least one of R2, R2', R3 and R3' must be OH. A pharmaceutical composition thereof is useful for treating infections, infestations, neoplasm, or autoimmune diseases or for modulating Th1 and Th2 activities in a patient.
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