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Progenitors of Anti-Tubercular and Antiviral Preparations

#G-1620


Progenitors of Pirrolo Coumarine Triciclice Condensed Systems with Antiviral Activity and for the Struggle against Tuberculosis (Synthesis and Wide Screening)

Tech Area / Field

  • BIO-CGM/Cytology, Genetics and Molecular Biology/Biotechnology
  • MED-DID/Diagnostics & Devices/Medicine

Status
3 Approved without Funding

Registration date
01.04.2008

Leading Institute
Georgian Technical University, Georgia, Tbilisi

Collaborators

  • Southern Research Institute, USA, AL, Birmingham

Project summary

The statistical data on the present day global "tuberculosis problem" are well known: one-third of the world’s population is considered infected; 6 million new cases are registered every year; tuberculosis accounts for 20% of adult and 6% of infant deaths. The increasing resistance of tuberculosis to drugs certainly highlights the need for creating new antitubercular drugs.

Likewise important is a need for creating new antiviral agents.

Among a countless number of compounds the bicyclic system of coumarine (5,6-benzo-α-pyrone) is regarded as the most promising one for a successful struggle with tuberculosis.




This optimism is based on a wide range of the pharmacological action which is characteristic of the derivatives of this simple bicyclic system. In particular we should note their capacity to inhibit the spread of viruses as well as their local anaesthetizing and analgetic capacities. Alkyl-substituted coumarines inhibit the growth of or stumulate the germination of seeds. The alcoholic extract of Peucedanum ostruthium root (Umbelliferae family) is used to treat digestive disturbances and typhoid fever; it is also used as a diuretic and for treating agricultural cattle.

Special interest is shown in the anticoagulative, spasmolytic, antitumoral and other properties of coumarines.

As the second system we have chosen indole the derivatives of which are also characterized by a variety of physiological activity.

Tricyclic systems, unsubstituted indoles and their dioxoderivatives with a coumarine fragment in the molecule are synthesized using 6-aminocoumarine. As substitutes we will choose the residues of semi- and thiosemicarbazides, hydrazides of nicotinic and isonicotinic acid, hydroxylamine, hydrazinehydrate, amino acids, alkylamines, sulfonic acids and so on, i.e. we will introduce the substitutes which, according to our data, favor the biological activity of the molecule as a whole.

All the synthesized compounds will be characterized by the modern analysis methods (IR, UV, NMR spectroscopy and mass-spectrometry).

The constant perfection of the methods of synthesis of starting products will make it possible to raise the yield of target products to an optimal level.


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