abstract |
Compounds of the formula I: n n n where; n R 1 is O, S; n R 2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; n R 3 is H, C 1 -C 3 alkyl, n R 4 -R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, haloC 1 -C 6 alkyl, C 1 -C 6 alkanoyl, haloC 1 -C 6 alkanoyl, C 1 -C 6 alkoxy, haloC 1 -C 6 alkoxy, C 1 -C 6 alkyloxy-C 1 -C 6 alkyl, haloC 1 -C 6 alkyloxy-C 1 -C 6 alkyl hydroxy-C 1 -C 6 alkyl, amino-C 1 -C 6 alkyl, carboxy-C 1 -C 6 alkyl, cyano-C 1 -C 6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; n X is —(CHR 8 ) n- —D—(CHR 8 ) m —; n D is —NR 9 —, —O—, —S—, —S(═O)— or —S(═O) 2 —; n R 8 is independently H, C 1 -C 3 alkyl, halo substitutedC 1 -C 3 alkyl; n R 9 is H, C 1 -C 3 alkyl; n n and m are independently 0, 1 or 2; n and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants. |