| abstract |
"NON-NUCLEOUS REVERSE TRANSCRIPTASE INHIBITORS". The present invention relates to compounds of formula Ar¬ 1¬-XW-Ar¬ 2¬ where Ar¬ 1¬ and Ar¬ 2¬ represent aryl groups generically characterized as aromatic heterocycles (e.g., imidazolyl or tetrazolyl) or carbo cycles. (e.g. phenyl or naphthalenyl); aryl groups are optionally substituted or fused to other heterocycles or crocycles; aryl groups may carry substituents such as alkyl, halo or O-alkyl. X is a heteroatom, valence bond or optionally substituted divalent methylene and W represents a spacer; Typical spacers include divalent alkylene or alkylene starch, starch or oxide radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a 2- (N-naphthalenyl tetrazolylthio) -N- (2-nitrophenyl) acetamide derivative. The compounds have inhibitory activity against wild-type strains and single or double HIV mutants. |