![]() |
![]() |
||||||||||||
|
02515 HIGH-EFFICIENT MEMBRANE-ACTING NORBORNENE- AND NORBORNANE-CONTAINING ANTI-HIV MICROBICIDES Perminova N.G. More than 90% of new cases of HIV-infection occur via heterosexual route; as a consequence, HIV-1/2 is quickly spread among women. Because of this, the development of efficient local remedies for prevention of HIV infection is undoubtedly urgent. As we demonstrated previously (Timofeyev D.I. et al., 2003), membrane-acting compounds based on polycarboxyacilic matrix and norbornene exhibit high anti-HIV activity toward different strains of HIV-1 and in different virus-cell systems at early stages of interaction; because of this, they can be proper candidates for designing a high-efficient microbicide preparation on this basis. We synthesized a series of compounds of matrix-norbornene type differing by matrix structure, hydrophobic-hydrophilic balance of norbornene derivatives, framework structure of membrane-acting modifier, length of spacer groups and stereo isomerism of modifiers (exo/endo versions of norbornene); we evaluated toxicity and antiviral activity of these compounds. Taking into account the above-listed parameters, we chose an optimal chemical structure of the complex compound providing the highest level of anti-HIV efficiency in the in vitro system for the purpose of perspective development of microbicide preparation for local intravaginal application. Dr. Nataliya Perminova |
|||||||||||||