Bioorganic and Medicinal Chemistry Group

The research of the Bioorganic and Medicinal Chemistry Group is mainly focused on pharmaceutical (medicinal) chemistry of the compounds with potential antimicrobial activities. Based on current knowledge in this particular field, we design and synthesize selected compounds of various chemical structures and study their structure-activity relationships with respect to antimicrobial activity, cytotoxicity and selectivity. In cooperation with several research groups, we study the mode of action of our compounds. The majority of the studied compounds with antimicrobial activities belong to the group of salicylanilides and salicylic derivatives, isoniazid analogues, nitrogen heterocycles and nitro group-containing compounds.

Second line of our research is focused on the structure-activity relationships of dexrazoxane, the only approved drug capable of preventing anthracycline-induced cardiotoxicity both in experimental models and clinical practice. As a part of this research, we also study the acylhydrazone-type and thiosemicarbazone-type iron chelators.

Additionally, we investigate also potential inhibitors of acetylcholinesterase and butyrylcholinesterase, especially those based on carbamate moiety and phenolic derivatives.

We are open to collaborations in those areas of research; feel free to contact us.

News

  • 22 July 2021 - PCT patent application (WO2021/144746 A1 "Use of ICRF-193 derivatives and pharmaceutical preparations containing thereof for the prevention of chronic cumulative cardiotoxicity caused by therapy with anthracycline anticancer drugs" has been published
  • February 2021 - our Czech Health Research Council project NU21-05-00446 From hit-to-lead candidate – development of novel agents to combat tuberculosis (May 2021-2024) has been funded
  • December 2020 - our Czech Science Foundation project 21-16195SChemical biology approach to study anthracycline cardiotoxicity and pharmacological cardioprotection with focus on topoisomerase II beta (2021-2023) has been funded
  • Ph.D. positions available (both in Czech and English language; starting in October 2021, applications are accepted until April 30, 2021)

Topics:

1. Synthesis of substituted nitrogen heterocycles with potential antimycobacterial activity
2. Synthesis of analogues of clinically used cardioprotective drug dexrazoxane and study of their structure-activity relationships
3. Structure-activity relationship study of potential topoisomerase II inhibitors

4. Synthesis and evaluation of potential antimycobacterial agents

5. Synthesis and evaluation of compounds active against drug-resistant Gram-positive cocci

For more information click here

 

  • November 2020 - CZ Patent No. 308 557 "Substituted 1,2,4-oxadiazole, its use and pharmaceutical preparation containing the same" has been granted
  • December 2018 - Svenox Pharmaceutical LLC bought the property rights to our

    application for invention No. PV 2018 – 664 entitled "Substituted 1,2,4-oxadiazole, its use and pharmaceutical preparation containing the same"

  • November 2018 - Jaroslav was awarded by the Alfred Bader’s Prize in bioorganic and bioinorganic chemistry

Diploma

 

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