At SPbU, Tetrazoles and Other Polinitrogen Heterocycles for Biomedicine is well underway. The research project, supported by the grant of the Russian Science Foundation, focuses on the organic compounds to increase the drug efficiency and make them less toxic.

Today, developing our original drugs produced in Russia is an overarching priority in Russian science. By using research advances in drug production and developing Russian analogues of the foreign drugs used in treatment and diagnostics of cardio-vascular diseases, diabetes, infectious diseases, cancer and others, we can increase life quality and expectancy and make Russia independent from the foreign drugs.

The drug production comprises a number of obligatory and time-consuming stages of the laboratory research. How much time and money is necessary depends on how the lead-compound, a base of the drug, is constructed. One of the most effective and value-for-money method is Analogue-based Drug Discovery.

The method implies that the analogue of an existing drug and/or natural molecules shares chemical and therapeutic similarities with the original compound, but comprises artificial fragments slightly different from their prototypes. The analogue can be more effective that the original compound. The method helped develop highly effective drugs that are the global market leaders now and have a lion share in the income of big pharmaceutical companies.

By incorporating these heterocyclic fragments through chemical synthesis into the biologically active substances, we can increase their efficiency (up to hundred or thousand times) and reduce their toxicity, said SPbU’s Professor Rostislav Trifonov.  These methods, however, are limited.

Chemistry has lots of questions to answer, but Russian scientists who have been working with polinitrogen heterocycles, are well ahead of their foreign counterparts in a number of areas.
SPbU’s Professor Rostislav Trifonov

“We are planning to reinforce this trend by carrying out our research on the synthesis, structure and biological activity of the polinitrogen heterocycles that are potential drugs”— said Rostislav Trifonov.

As a rule, pharmacophores, key biologically active fragments of the drugs, are functional groups that are rarely found or even never occur in nature. Such fragment is a tetrazolium cycle and five-membered nitrogen heterocycles, which are similar in structure with tetrazolium cycles, containing three or more  endocyclic heteroatoms.

In their research, SPbU’s scientists use cutting-edge technologies of the fine organic synthesis and physical-chemical analysis. Mostly, the research is carried out at the SPbU’s Resource Centres.

The research group headed by Rostislav Trifonov comprises experts in chemistry of nitrogen heterocycles, chemistry of natural compounds, pharmaceutical chemistry, SPbU’s young scientists, students, and academic staff of the St Petersburg State Institute of Technology. Further, it will attract chemists and biologists from other institutions.