Inhibition of HIV-1 replication using oligocarbamate derivatives

Details Inhibition of HIV-1 replication using oligocarbamate derivatives Inhibition of HIV-1 replication using oligocarbamate derivatives

1997-07-07

1998-12-01

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

560 24, A61K 3124, C07C20516

Patent

active

058439951

ABSTRACT:
Tat-inhibitory oligocarbamate derivatives of the formula I ##STR1## and analogs thereof, and the biologically and pharmaceutically acceptable salts thereof exhibit advantageous properties, including specific binding to TAR RNA with high affinities, and stability of the resultant oligocarbamate-RNA complexes to proteolytic digestion. Site-specific photocrosslinking experiments using a photoactive analog (4-thio-uracil) containing TAR RNA indicate that these oligocarbamates interact with RNA in the major groove. These oligocarbamates are thus capable of competing with the TAR RNA-binding domain of Tat protein and thus are useful as a therapeutic agents in the treatment of AIDS.

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