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Medical Heterocyclic Compounds


Synthesis and Study of Some Groups of Heterocyclic Compounds having Cardiovascular, Immunolmodulating and Antiviral Effects

Tech Area / Field

  • BIO-CHM/Biochemistry/Biotechnology
  • MED-DRG/Drug Discovery/Medicine

3 Approved without Funding

Registration date

Leading Institute
Scientific Research Institute of Vaccines and Sera, Russia, St Petersburg

Project summary

The objective of this project is to develop new more effective medicinal preparations for the treatment and prophylactic of cardiovascular and immunodeficient diseases. These diseases are widely spread in many countries of the world. According to literature data the highest per cent of death is caused by cardiovascular diseases and immunodeficient diseases especially AIDS, considered "the Black Death" of the XXth century. Therefore, in many leading scientific research centers intensive efforts are made to develop new highly effective preparations for the treatment and prophylactic of the above diseases.

To achieve the purpose delivered in the given project, many derivatives of heterocycles important in terms of biology will be synthesized and studied, such as benzopyran-2-on, imidazole, benzimidazole and some nucleic bases; the most active compounds will be selected and their specific pharmacological properties will be studied in accordance with the requirements of the Pharmacology Committee of the Russian Federation; relevant medicinal forms of the products under development will be created and a scientific technical documentation will be compiled including experiment and production regulations (EPR), provisional pharmacopoeia articles (PPHA), projects of instructions on the use of the products under development and their experimental series for clinical tests. In order to perform the above stages of activities, the most reliable and modern methods of classic organic chemistry will be used, in particular, IR-and NMR-spectroscopy and chromatomass spectrometry. Efficiency of the compounds under study will be estimated on laboratory animals using routine pharmacological, immunopharmacologic and virology methods in accordance with GLP.

Thus, as a result of the aforesaid activities, three original preparations are expected to be developed. They are: antiischemic preparation (Az-105) owning the properties of Ca++ antagonists which is the analogue of diumancale developed by us and approved in 1996 by the Pharmacology Committee of the Russian Federation for the treatment of heart ischemia (protocol N 10 of 27.06.96) as well as patented in Russia (N 1827066,1992); immunomodulator Az-26 and antiviral preparation Az-48 (heterovir) for the treatment and prophylactic of immunodeficient diseases. The above compounds have a pronounced pharmacological activity and substantially (3-5 fold) surpass the known analogues such as nifedipine, verapamile, diltiazem, levamisole, amantadine, rimantadine and virasole.

In conclusion, it should be noted that the proposed project and the scientific research trend, which we have developed for many years are supported by many foreign colleagues, in particularly Dr.Rodney W.Nichols, President of the New-York Academy of Sciences, by Professor Norbert D.Kimpe, Head of the Organic Chemistry laboratory of Belgium University, as well as by the pharmaceutical companies OSIRIDE in Milan (President R.Maggi), PANAX in New-York (President Taffy Williams) and other firms. With these authors we have got the mutual publications and patents concerning the approaches and methods of international standardization and certification as well as of commercialization of the results obtained from the development of new medicinal preparations. Therefore, we expect their participation in the fulfillment of the project and in the realization of its results.

We are also ready to cooperate with other foreign scientists and firms working in the field of creation the medicinal preparations having cardiovascular, immunomodulating and antiviral effects. We have perfect base for synthesis and analysis, study the specific pharmacological activity and nontoxic, creation of relevant medicinal form, study pharmacokinetics and bioavailability of developing preparations. We are interested in the establishment of cooperation and realization of our original development (new substances, medicinal preparations and technologies).


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