Main results 2012

1. USNIC ACID DERIVATIVE WITH REMARKABLE BIOLOGICAL ACTIVITY

New bioactive compound Thiazol® was synthesized from natural usnic acid.

Our colleagues from the Laboratory of Genetics of microorganisms Vavilov Institute of General Genetics revealed that Thiazol® possesses bacteriostatic activity against clinical MDR strain M.tuberculosis MS-115 in the minimum growth inhibitory concentration - 5 µg/ml.

Thiazol differs from drugs used in the traditional medicine by the mode of action, act as an inhibitor of M. tuberculosis oxidative phosphorylation.

According to the research is concluded a State Contract 12411.1008799.13.002 (2012) “Preclinical studies of anti-tuberculosis drugs on the basis of semi-synthetic derivatives of usnic acid”.

2. СNEW SPIN LABELED BIOACTIVE NATURAL COMPOUNDS AS AN AGENTS FOR MRI

3. Stable polyfluoroaromatic zinc derivatives.

For the first time bis(zinc)perfluorophenylenes were synthesised. The unique technology allows to prepare reactive organometal intermediate from 1,4-dibromotetrafluorobenzene. This intermediate can be used for synthesis of symmetric perfluoroaryl derivatives – monomers for production of materials of special destination.

4. Polynitrogen heterocyclic ligands for multifunctional materials

5. BIOLOGICALLY ACTIVE DERIVATIVES OF SESQUITERPENE LACTONES BY PALLADIUM CATALYSED CROSS-COUPLING REACTIONS

Using sesquiterpene methylene lactones of eudesmane type as an alkene component in the Heck reactions we developed a new methodology to the arylated lactones with an active methylene function. On the base of this approach several hybrid molecules containing the fragments of methylene lactones and diterpene or quinazoline alkaloids were synthesized. We mentioned a number of compounds very interesting from the biological point of view. Among 13-arylsubstitutedderivatives of isoalantolactone selectively acting antiulcer agents were discovered.