| abstract |
In the present invention, there are disclosed HIV protease novel inhibitors comprising substituted borane, carborane or metallacarborane clusters having 6 to 12 boron atoms in each individual cluster, wherein charge of each individual borane, carborane or metallacarborane cluster is 0. -1 or -2. The borane, carborane or metallacarborane clusters are substituted on periphery with groups increasing interaction energy between HIV protease and the inhibitor, wherein number of the borane, carborane or metallacarborane clusters in the inhibitor molecule ranges from 1 to 9, wherein the carborane clusters in the metallacarborane inhibitors are coordinated to a transient metal atom being selected from the group consisting of Co, Fe, Ni and Ru. Disclosed is also the use of these inhibitors in vitro as well as in vivo. Introduction of the derivative of the boron cluster compounds as a novel structural element provides inhibition properties for HIV protease and mutants thereof that are resistant to other inhibitors. Low toxicity, stability and biocompatibility along with high efficiency make these boron compounds suitable for AIDS therapy. |