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Львівський національний медичний університет

Головна / University / Departments / Фармацевтичний факультет / Department of pharmaceutical, organic & bioorganic chemistry

DEPARTMENT OF PHARMACEUTICAL, ORGANIC AND BIOORGANIC CHEMISTRY

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Address
79010, UKRAINE, Lviv, Pekarska str., 69.
phone +38 (0322) 75-59-66, 75-59-77, 786-434
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Head of Department:
Lesyk Roman  

 

Staff:

  • Prof. Zimenkovsky Borys DSc, PhD;
  • prof. Muzychenko Volodymyr DSc, PhD;  
  • prof. Lesyk Roman DSc, PhD;
  • associate prof. Horishny Volodymyr PhD; 
  • associate prof. Kaminskyy Danylo PhD; 
  • associate prof. Semenciv Hryhory PhD; 
  • associate prof. Shtojko Natalya PhD; 
  • associate prof. Demchuk Inna, PhD; 
  • associate prof. Zelisko Natalya PhD; 
  • associate prof. Kryshchyshyn Anna PhD;
  • senior lecturer Gavryliuk Olha, PhD; 
  • senior lecturer Grabovyj Petro, PhD; 
  • senior lecturer Novikevych Оlha, PhD; 
  • senior lecturer Lebjak Мyhaylo PhD; 
  • assistant prof. Lozynskyi Andrii PhD;
  • assistant prof. Subtel'na Ivanna PhD;
  • assistant prof. Ivanciv Oksana;
  • assistant prof. Vovchyk Orysja;
  • PhD students: Wojtyra M.

EDUCATIONAL WORK

Main directions of scientific research:

Scientific investigations are performed in the area of synthesis, chemical modifications and biological activity studies of the heterocyclic substances among 4-azolidone, 1,3-thiazane, thiazolothiopyran derivatives, introduction of innovational approaches to drugs design (QSAR-analysis, virtual screening, molecular modeling, molecular docking). They are the continuation of the scientific school of professors M. Turkevych, O. Vladzimirska and B. Zimenkovsky. Since 1946 students’ scientific group works at the department.

Main scientific achievements:

Six new drugs were introduced in medical practice at the department (penthabismol, dimexide, trichloroethylene for narcosis, diamiphene, fluorenizide, thiotriazoline). Over 100 author certificates on inventions are obtained. There were 27 Doctors of Sciences and over 100 Candidates of Sciences (PhDs) studied and defended their theses at the department.
Joint scientific investigations with the group of Ukrainian and foreign scientific institutions allowed us to formulate the strategy of purposeful search of new potential drugs among the group of 4-azolidones and related heterocyclic systems. As a result of high-throughput and traditional pharmacological screening more than 200 “lead-compounds” have  been identified with з anticancer, anti-inflammatory, antioxidant, anti-ischemic, cerebral-protective antimicrobial, antifungal and antituberculosis activities. For the 4-azolidone derivatives anticancer activity have been identified for the first time that shows the novelty and investigation priority of mentioned class of compounds. Advanced pharmacological studies of potential cerebroprotectants had been performed in collaboration with Dept. of Pharmacology of Lugansk State Medical University. New areas of nowel “drug-like” molecules search have been explored, namely search of antiviral and anti-trypanosomal agents.
 Using the materials of our investigations the row of monographs has been published, among which are “4-Thiazolidones. Chemistry, physiological action, perspectives ” (authors B.S. Zimenkovsky, R.B. Lesyk), as well as fundamental review “4-Thiazolidones: Centenarian History, Current Status and Perspective for Modern Organic and Medicinal Chemistry” (authors B.S. Zimenkovsky, R.B. Lesyk) in the journal “Current Organic Chemistry”, a series of original articles in foreign and Ukrainian journals, such as Bolletino Chimico Pharmaceutico, Scientia Farmaceutica, Journal of Pharmacy and Pharmacology, Bioorganic and Medicinal Chemistry, Polish Journal of Pharmacology, Acta Poloniae Pharmaceutica – Drug Research, Annals of Polish Chemical Society, Ukrainica Bioorganica Acta, Journal of pharmaceutical and organic chemistry (in Ukrainian), Pharmaceutical Journal (in Ukrainian) etc. Our research yielded in over 30 Ukrainian patents obtained for novel biologically active compounds and methods of their synthesis.

Scientific collaboration

  1. National Cancer Istitute of National Institute of Health (Bethesda, Maryland, USA) under the screening program of anticancer activity for original compounds (Developmental Therapeutic Program). – http://dtp.nci.nih.gov
  2. National Institute of Allergic and Infectious Diseases of National Institute of Health (Bethesda, Maryland, USA) – screening of antituberculosis and antiviral activities under the TAACF and AACF programs. – http://www.taacf.org; http://www.aacf.org
  3. National Institute of Neurological Diseases and Stroke of National Institute of Health (Bethesda, Maryland, USA) – screening of anticonvulsant activity – Anticonvulsant Drug Development Programm. – http://www.ninds.nih.gov
  4. Karol Marcinkowski Poznan University of Medical Sciences (Poland) – agreement about joint research and young scientists exchange in the areas of the drugs search, anticancer activity and cytotoxicity assays of active compounds. – http://www.amp.edu.pl
  5. University of Southern Denmark (Odense, Denmark), Department of Chemistry (Prof. Frank Jensen) – joint research in rational structure design and molecular modeling of potential drugs. – http://www.sdu.dk
  6. Collegium Medicum of Jagellonian University (Krakow, Poland), Department of Chemical Technology and Biotechnology of Drugs (prof. Katarzyna Kiec-Kononowicz) – joint research in the ares of search of new drugs amond group 4-azolidones. – http://www.cm-uj.krakow.edu.pl
  7. Lugansk State Medical University (prof. V.D. Lukjanchuk) – antioxidant, anti-ischemic and cerebro-protectant activities assays for newly synthesized compounds. - http://www.lsmu.com
  8. F. Skubiszewski Academy of Medical Sciences (Lublin, Poland). Department of Organic Chemistry, Department of Toxicology – PhD studies of our university alumni. - http://www.am.lublin.pl
  9. Maria Sklodowska-Curie University (Lublin, Poland), Department of General Chemistry – synthesis of complex compounds of biometals with N,S,O-donating ligands with biological activity, physico-chemical activities studies of synthesized compounds. Biological activities assays of complex substances. – http://www.umcs.lublin.pl
  10. Bogatsky Physico-chemical Institute of NAS of Ukraine (Senior researcher A.H. Artemenko)

Main publications

  1. D. Havrylyuk, B. Zimenkovsky, O. Vasylenko, Andrzej Gzella, R. Lesyk Synthesis of New 4‑Thiazolidinone‑, Pyrazoline‑, and Isatin-Based Conjugates with Promising Antitumor Activity // J. Med. Chem.,2012, 55, p. 8630−8641.
  2. B. Zimenkovsky, О. Vladzimirska, R.Lesyk. Doctor of Technical and Pharmaceutical Sciences, Professor Mykola Turkevych - an outstanding scientist in the field of pharmaceutical chemistry. To the 100th anniversary of his birth. Lviv, 2012. – 112p. (In Ukrainian).
  3. D. Kaminskyy, D. Khyluk,O. Vasylenko,R. Lesyk. An efficient method for the transformation of 5-ylidenerhodanines into 2,3,5-trisubstituted-4-thiazolidinones // Tetrahedron Lett., 2012, 53(5), p.557-559.
  4. Anna Kryshchyshyn, Dmytro Atamanyuk, Roman Lesyk. Fused thiopyrano[2,3-d]thiazole derivatives as potential anticancer agents / Sci.Pharm., 2012, 80(3), p.509-529.
  5. Nataliya Zelisko, Dmytro Atamanyuk, Olexandr Vasylenko, Philippe Grellier, Roman Lesyk. Synthesis and antitrypanosomal activity of new 6,6,7-trisubstitutedthiopyrano[2,3-d][1,3]thiazoles // Bioorgan. Med. Chem.Lett., 2012, 22(23), p. 7071-7074.
  6. Danylo Kaminskyy, Barbara Bednarczyk-Cwynar, Olexandr Vasylenko, Oxana Kazakova, Borys Zimenkovsky, Lucjusz Zaprutko, Roman Lesyk. Synthesis of new potential anticancer agents based on 4-thiazolidinone and oleanane scaffolds // Med. Chem. Res., 2012, 21(11), p. 3568-3580.
  7. D. Kaminskyy, D. Khyluk, O. Vasylenko, R. Lesyk. An efficient method for the transformation of 5-ylidenerhodanines into 2,3,5-trisubstituted-4-thiazolidinones // Tetrahedron Lett.,2012, 53(5), p. 557-559.
  8. D. Kaminskyy, D. Khyluk, O. Vasylenko, L. Zaprutko, R. Lesyk. A Facile Synthesis and Anticancer Activity Evaluation of Spiro[Thiazolidinone-Isatin] Conjugates // Sci.Pharm., 2011, 79(4), p.763-777.
  9. Lesyk R.B., Zimenkovsky B.S., Kaminskyy D.V., Kryshchyshyn A.P., Havryluk D.Ya., Atamanyuk D.V., Subtel’na I.Yu., Khyluk D.V. Thiazolidinone motif in anticancer drug discovery. Experience of DH LNMU medicinal chemistry scientific group // Biopolymers and cell, 2011, 27(2),p. 107-117.
  10. Dmytro Havrylyuk, Ludmyla Mosula, Borys Zimenkovsky, Olexandr Vasylenko, AndrzejGzella & Roman Lesyk. Synthesis and anticancer activity evaluation of 4-thiazolidinones containing benzothiazole moiety // Eur. J. Med. Chem.,2010, 45, p. 5012-5021.
  11. D. Havrylyuk, N. Kovach, B. Zimenkovsky, O. Vasylenko, R. Lesyk. Snthesis and Anticancer Activity of Isatin-Based Pyrazolines and Thiazolidines Conjugates // Arch. Pharm. Chem. Life Sci., 2011. 344№8. -P.514–522.
  12. D. Kaminskyy, O. Vasylenko, D. Atamanyuk, A. Gzella, R. Lesyk. Isorhodanine and thirhodanine motifs in the synthesis of fused thiopyrano[2,3-d][1,3]thiazoles // SYNLETT. –2011. -10. –P.1385-1388.
  13. I. Subtelna, D. Atamanyuk, E. Szymańska, K. Kieć-Kononowicz, B. Zimenkovsky, O. Vasylenko, http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF8-508K803-1&_user=10&_coverDate=06%2F09%2F2010&_rdoc=1&_fmt=high&_orig=search&_sort=d&_docanchor=&view=c&_acct=C000050221&_version=1&_urlVersion=0&_userid=10&md5=05f1770701908a639b405ae74b80d237 - aff3A. Gzella, R. Lesyk. Synthesis of 5-arylidene-2-amino-4-azolones and evaluation of their anticancer activity // Bioorg. Med. Chem. –2010. –vol.18(14). –P.5089-5101.
  14. D. Havrylyuk, B. Zimenkovsky, O. Vasylenko, L. Zaprutko, A. Gzella, R. Lesyk. Synthesis of novel thiazolone-based compounds containing pyrazoline moiety and evaluation of their anticancer activity //Eur. J. Med.Chem., 2009, 44(4), p. 1396-1404.
  15. D.Havrylyuk, B.Zimenkovsky, R.Lesyk. Synthesis and Anticancer Activity of Novel Nonfused Bicyclic Thiazolidinone Derivatives //PhosphorusSulfur, 2009, 184, p.638-650.
  16. D. Kaminskyy, B. Zimenkovsky, R.Lesyk. Synthesis and invitro anticancer activity of 2,4-azolidinedione-acetic acids derivatives // Eur. J. Med.Chem.,2009, 44(9), p.3627-3636.
  17. D. Atamanyuk, B. Zimenkovsky, R. Lesyk. Synthesis and anticancer activity of novel thiopyrano[2.3-d]thiazole-based compounds containing norbornane moiety // J. Sulf. Chem., 2008, 29(2), p.151-162.
  18. V. Matiychuk, R. Lesyk, M. Obushak, A. Gzella, D. Atamanyuk, Yu. Ostapiuk, A. Kryshchyshyn. A new domino-Knoevenagel-hetero-Diels-Alderreaction // TetrahedronLett., 2008, 49(31) p.4648-4651.
  19. Zimenkovsky B.S., Lesyk R.B. 4-Thiazolidones. Chemistry, physiological action, perspectives. Monograph. Vinnytsia: Nova Knyga, 2004. –106p. (In Ukrainian)
  20. I.A. Mazur, Voloshyn N.A., I.C. Chekman, B.S.Zimenkovsky, V.R. Stec. Thiotriazoline. Pharmacological aspects and applications. Nautilus, Lviv. -2005. -146p. (In Russian)
  21. Roman Lesyk & Borys Zimenkovsky. 4-Thiazolidones: Centenarian History, Current Status and Perspectives for Modern Organic and Medicinal Chemistry // Current Organic Chemistry –2004. –Vol.8, №16.  –P.1547-1578.
Disciplines, taught at the department:
  • Bioorganic Chemistry
  • Organic Chemistry
  • Pharmaceutical Chemistry
  • Medicinal Chemistry
  • Standardization of Drugs
  • Innovations and Intellectual Property Protection
  • Computer Technologies in Pharmacy
  • Specializations:
  • Drugs Development
  • Standardization of pharmaceutical production
  • Elective courses:
  • Theoretical basis of synthesis and “structure-activity” relationships of drugs
  • Spectral investigations of drugs and physiologically active substances

Academic instruction:

Bioorganic chemistry is studied for the 1st year students of medical and dentistry faculties and for 2nd year students of pharmaceutical faculty.
Organic chemistry is studied for the pharmaceutical faculty students of 2nd year.
Pharmaceutical chemistry is studied at 3rd-4th years for the students of pharmaceutical faculty (“Pharmacy” direction).
Medicinal chemistry is studied for the 3rd-4th years students of pharmaceutical faculty (“Clinical Pharmacy” direction).
During the 4th and 5th year of pharmaceutical faculty tuition there are studied newly introduced courses “Standardization of drugs”, “Innovations and intellectual property protection”, “Computer technologies in pharmacy”.
At lectures and practical classes students study drugs, methods of their synthesis and analysis, standardization, particulars of structure and action of modern drugs.

 

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