Progenotors for Antiviral and Tuberculostatic Preparations
Investigation by Prof. T.Khoshtaria's Method of the Synthesis of 1H-Benzo[B]Thiophen(Furo)-Indoles and 1H-Benzo[B]Thiophen(Furo)-Benzimidazoles with Antiviral and Tuberculostatic Activities (Synthesis And Wide Screening)
Tech Area / Field
- BIO-CGM/Cytology, Genetics and Molecular Biology/Biotechnology
- MED-DID/Diagnostics & Devices/Medicine
3 Approved without Funding
Georgian Technical University, Georgia, Tbilisi
- Southern Research Institute, USA, AL, Birmingham\nErweiterte Realschule Saarbrücken -Güdingen, Germany, Saarbrücken
Project summaryThe basic statistics of the present-day global tuberculosis problem are well known: one-third of the global population is considered infected; 6 million new cases each year; 20% of adult death and 6% of infant deaths are attributable to TB… there is the urgent need for new drugs… (Patrick J. Brennen. Plenary lecture. International Symposium on Current Developments in Drug discovery for Tuberculosis, Bangalore, India, 2002).
The search for new preparations against tuberculosis has not so far brought any better results than Isoniazid®, Phtivazid® and their derivatives – compounds synthesized many years ago. One of the most serious problems in the chemotherapy of tuberculosis is the bacterial resistance to the currently used drugs. The development and application of principally new types of preparations remain still topical to solve this problem.
Among a large variety of chemical compounds with potential antitubercular activity there are derivatives of indole, especially dioxodihydro-1H-benzo[b]furoindoles, the tetracyclic systems which were synthesized for the first time by the Georgian team and which can be considered as ones of the most (if not the most) promising compounds in combating this disease. This optimism is based on the high antituberculostatic activity revealed by these heterocyclic systems and their derivatives.
Therefore the project participants will focus their effort on the synthesis of antitubercular compounds, the more so that tuberculosis is a problem not only for Georgia.
The basic heterocyclic condensed systems – indole-containing [b]-annulated benzofurans synthesized earlier by the Georgian team of researchers (led by Prof. T. Khoshtaria) will be the “leading compounds” in producing new target products that are also expected to possess a tuberculostatic effect.
Below, the properties of indole and indole-containing tetracyclic systems, and their derivatives – both of natural and of ynthetic origin – are briefly discussed to elucidate the importance of the problems and tasks of the present project.