Laboratory chemical transformation of antibiotics

The department was established in 1987 by Professor Maria N. Preobrazhenskaya, who directs the Laboratory from 1987 to 2015. The department is a successor of the Group of Semisynthetic Antibiotic Derivatives organized in 1975 by D.Sc. L.S. Povarov and directed by him until 1987. Currently, the lab is headed Dr. Sci, Professor Andrey E. Shekotihin

Staff: Evgenia N. Olsufjeva, Dr. Sci, Professor; Alexander M. Korolev, Dr. Sci; Andrey E. Shekotihin, Dr. Sci, Professor; Svetlana S. Prinzevskaya, Ph.D.; Victor B. Zbarskij, Ph.D.; Marina I. Reznikova, Ph.D.; Sergey A. Lakatosh Ph.D.; Sergey N. Lavrenov, Ph.D.; Yuryi N. Luzikov, Ph.D.; Lubov G. Dezhenkova, Ph.D.; Evgeniy Bykov, Ph.D.; Anna N. Tevyashova, Ph.D.; Svetlana E. Solovyeva,, Ph.D.; Mrs. Elena N. Bychkova; Mrs. Natalia M. Maliutina; Alexander J. Simonov, , Ph.D.; Mr. Alexander S. Tikhomirov

Main Research Areas:

  • Studies on semisynthetic derivatives of antibacterial and antiviral glycopeptide antibiotics.
  • Studies of semisynthetic derivatives of cytotoxic antibiotics (anthracyclines, streptonigrine, olivomycin, oligomycin and some others). Studies of semisynthetic derivatives of antifungal polyene antibiotics.
  • Synthesis and study of structure-activity relationships in heteroareneanthraquinones.
  • Chemical modification and structure-activity relationships of antibiotic derivatives and other natural compounds active against tumor or bacterial cells with different types of drug resistance.
  • Studies on ascorbigen and the products of its biotransformations.
  • Studies on bis-indolylmaleimides - new analogs of natural bis-indolylmaleimideantibiotics and indolocarbazoles. Studies of compounds containing tris(indol-3-yl)methyl moiety
  • Quantum chemical investigations of the structure and reactivity of the biologically active compounds.

Major Achievements:

  • Main directions of selective chemical transformations of antibacterial glycopeptides antibiotics have been developed; series of derivatives active towards vancomycin-sensitive and vancomycin-resistant strains of gram-positive bacteria have been prepared.
  • A novel mechanism of activity of hydrophobic glycopeptide derivatives against vancomycin-resistant gram-positive bacteria has been proposed. This mechanism does not depend on the interaction with vancomycin target in Gram-positive bacteria, which is altered in resistant bacterial cells.
  • Antiviral activity of antibacterial glycopeptide derivatives against several enveloped viruses ( HIV, VZV, HSV, SARS and others) has been demonstrated.
  • Analogs of natural bis-indolylmaleimide antibiotics of a new type have been prepared; some of these analogs are strong inhibitors of bacterial or eukaryotic serine-threonine protein kinases.
  • Series of heteroareneanthraquinones targeted to topoisomerase-I and telomerase have been synthesized, these derivatives inhibit growth of tumors in mice with implanted tumors.
  • Methods of selective chemical modifications of natural and genetically modified antifungal polyene antibiotics were elaborated, some of new compounds were more active and less toxic than amphothericin B in neutrophilic mice infected with Candida albicans.
  • Methods of chemical modification of antitumor antibiotic olivomycin A were elaborated and novel antibiotic derivatives with high antitumor activity in vivo and lower toxicity in comparison with olivomycin A were obtained.
  • Methods of chemical modification of an inhibitor of ATP-ase Oligomycin A were developed.
  • Biotransformation of ascorbigen has been studied and it was shown, that ascorbigen is a powerful modulator of nonspecific immunity and had a protective effect against bacterial and viral infections. It is also capable of alleviating toxic effects of antitumor drugs.

Publications:

Since 2000, 85 papers in International and Russian journals have been published, including two monographs and 6 reviews. Fourteen patents for inventions have been filed for and received. For detailed information, please see the list of publications

Новая статья о дапоксетин инструкция по применению и противопоказаниях.

Scientific contacts:

  • Blokhin Cancer Center, Russian Academy of Medical Sciences (Moscow).
  • Vavilov Institute of General Genetics, Russian Academy of Sciences (Moscow).
  • Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences (Moscow).
  • Mendeleyev University of Chemical Technology (Moscow).
  • Moscow Lomonosov Academy of Fine Chemical Technology (Moscow).
  • Lomonosov Moscow State University, Department of Chemistry.
  • Research Centre for Biotechnology of Antibiotics BIOAN, Moscow.
  • Division of Medical Biochemistry. Innsbruck Medical University, Austria.
  • Rega Instituut, Katholieke Universiteit Leuven, Belgium.
  • Department of Biotechnology, Norwegian University of Science and Technology, Trondheim, Norway.
  • Dipartimento di Chimica Biologica. University of Padova, Italy.
  • Department of Molecular and Cell Biology. University of California at Berkeley. Berkeley, CA. USA.
  • Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taiwan, Republic of China.
  • School of Pharmacy, National Defense Medical Center, Taiwan, Republic of China.
  • ProQinase GmbH. Freiburg. Germany.
  • Department of Biochemistry, University of Debrecen, Debrecen, Hungary.
  • Microbiology and Tumor biology Center. Karolinska Institutet Stockholm, Sweden.
  • Lab. chimie Organique II-Glycochimie Université Claude Bernard - Lyon 1 FRANCE.

Contact information:

Gause Institute of New Antibiotics, Russian Academy of Medical Sciences, 11 Bolshaya Pirogovskaya Street, Moscow 119021, Russia Phone (7499) 245 3753, (7499) 246 0228; e-mail: shchekotikhin@mail.ru





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