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Pyrazine derivatives as potential drugs VII.
Janďourek, Ondřej ; Doležal, Martin (advisor) ; Kopecký, Kamil (referee)
Pyrazin derivatives as potential drugs VII. Ondřej Janďourek Tuberculosis is one of the biggest health problems in the world. The number of new cases is rising every day, especially in less developed countries. The other problem is drug resistant tuberculosis which is occurring more and more frequently. Consequently these circumstances lead to one solution - to find new compounds to treat this greasy disease. This work deals with synthesis of undocumented compounds in literature. The starting compound was 5-chloro-6- methylpyrazine-2,3-dicarbonitrile. The compounds were developed by aminodehalogenational reaction by substituted anilines. Final compounds were characterized by molecular weight, melting point, TLC, logP, elemental analysis, 1 H and 13 C NMR and IR. Compounds were tested in vitro testing on their biological activity - antimycobacterial, antifungal and antibacterial.
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Detection of Sap2 in the secretome of Candida albicans cell wall and secretory mutants
Kollárová, Nikola ; Janďourek, Ondřej (advisor) ; Konečná, Klára (referee)
Candidate: Nikola Kollárová Title of diploma thesis: Detection of Sap2 in the secretome of Candida albicans cell wall and secretory mutants Charles University, Faculty of Pharmacy in Hradec Králové, Department of Biological and Medicinal Sciences Complutense University of Madrid, Faculty of Pharmacy, Department of Microbiology II Study program: Pharmacy Backgound: The aim of this diploma thesis was to search for C. albicans proteins involved in the secretion of the secreted aspartyl proteinase 2 enzyme (Sap2) evaluating the ability to degrade BSA (bovine serum albumin) as a source of nitrogen in several cell wall and secretory mutants of C. albicans. The work was carried out at the Department of Microbiology II, Faculty of Pharmacy, Complutense University of Madrid. Methods: The supernatant samples of several Candida albicans mutants were tested by SDS-PAGE electrophoresis and stained. Bands corresponding to BSA were observed and compared to controls. The other method was counted with 96-well plate. Results: The correlation between optical density and degradation of BSA was observed. Some mutants with disability to degrade BSA were found in a pilot screening of the ability to degrade BSA using 96-well plate method. That fact was confirmed by SDS-PAGE electrophoresis. C. albicans mutants showing...
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Microbiological diagnostics of causative agents of infectious diseases associated with central venous catheter insertion
Hošková, Miroslava ; Konečná, Klára (advisor) ; Janďourek, Ondřej (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Subject of study: Specialist in laboratory methods Student: Bc. Miroslava Hošková Supervisor: RNDr. Klára Konečná, Ph.D. Title: Microbiological diagnostics of causative agents of infectious diseases associated with central venous catheter insertion Background: The purpose of the thesis is to provide a comprehensive insight into the issue of microbiological diagnosis of agents that cause central venous catheter related infectious processes. The primary objective of the thesis is to evaluate the frequency of occurrence of individual microbiological agents and draw a comparison between published reports and empirical findings. The secondary objective of the thesis is to consider the extent of central venous catheter microbial colonization, i.e., in how many cases of positive culture cultivation, their contamination or significant colonization have been determined, and eventually whether system catheter infection has been proved in correlation with the results of blood culture. Methods: One hundred and seventy-one central venous catheters from different inpatient departments were delivered to the microbiological section of hospital Nemocnice Boskovice s. r. o. for culture examination have been...
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Effectiveness of disinfectants for hygienic hand disinfection against clinically important strains of enterococci
Malíková, Martina ; Janďourek, Ondřej (advisor) ; Konečná, Klára (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Study program: Bioanalytical laboratory diagnostics in health care Candidate: Bc. Martina Malíková Thesis supervisor: PharmDr. Ondřej Janďourek, Ph.D. Consultant: RNDr. Irena Hanovcová, CSc. Title of diploma thesis: Effectiveness of disinfectants for hygienic hand disinfection against clinically important strains of enterococci Alcohol-based hand disinfectants for hygienic hand disinfection are a key tool for the control of nosocomial infections worldwide. The aim of this study was to verify the effectiveness of these products, which are used in healthcare facilities, against vancomycin-sensitive and vancomycin-resistant enterococci isolated from clinical materials. Testing of the efficacy of disinfectants was performed according to the Czech technical standard ČSN EN 1040 - Chemical disinfectants and antiseptics - Quantitative test using suspension to determine the basic bactericidal effect of chemical disinfectants and antiseptics - Test method and requirements (phase 1). We used the dilution method with a neutraliser for our testing. There were used a total of 35 strains of enterococci to determine efficacy, 12 of which were vancomycin sensitive (four E. faecium strains and eight E. faecalis...
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Peptide and amino acid derivatives of antimicrobial active compounds
Šulcová, Kateřina ; Krátký, Martin (advisor) ; Janďourek, Ondřej (referee)
This bachelor thesis is concerned with newly synthetized compounds which have potential to be used in treatment of microbial infections or contribute to synthesis of novel, more convenient compounds. At first, it deals with bacterial resistance and related facts. Then, it summarizes possible modifications of drugs to obtain novel bioactive substances or to improve properties of already known drugs. The thesis summarizes some new amino acid derivatives of antimicrobial active agents. First, it describes primaquine analogues where acylation of primary amino group seems to be promising for the antimalarial activity, then it summarizes promising compounds with antibacterial activity, e.g., derivatives of fluoroquinolones or curcumin with physiological and unnatural amino acids. Finally, it deals with antimycobacterial agents - salicylanilide derivatives for treatment of tuberculosis and antileprotic dapsone derivatives to increase its solubility. In conclusion, peptide and amino acid derivatives can be effectively used to increase activity or to modify disadvantageous properties of small molecules (e.g., toxicity or solubility issues). Keywords Amino acid derivatives, drug modification, microbial resistance, peptides, prodrugs
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Microbiological diagnostics of causative agents of infectious diseases associated with central venous catheter insertion
Hošková, Miroslava ; Konečná, Klára (advisor) ; Janďourek, Ondřej (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Subject of study: Specialist in laboratory methods Student: Bc. Miroslava Hošková Supervisor: RNDr. Klára Konečná, Ph.D. Title: Microbiological diagnostics of causative agents of infectious diseases associated with central venous catheter insertion Background: The purpose of the thesis is to provide a comprehensive insight into the issue of microbiological diagnosis of agents that cause central venous catheter related infectious processes. The primary objective of the thesis is to evaluate the frequency of occurrence of individual microbiological agents and draw a comparison between published reports and empirical findings. The secondary objective of the thesis is to consider the extent of central venous catheter microbial colonization, i.e., in how many cases of positive culture cultivation, their contamination or significant colonization have been determined, and eventually whether system catheter infection has been proved in correlation with the results of blood culture. Methods: One hundred and seventy-one central venous catheters from different inpatient departments were delivered to the microbiological section of hospital Nemocnice Boskovice s. r. o. for culture examination have been...
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Atypical mycobacteria as causative agents of human diseases
Králíková, Lenka ; Janďourek, Ondřej (advisor) ; Konečná, Klára (referee)
Charles University Faculty of Pharmacy in Hradec Kralove Department of Biological and Medical Sciences Study program: Specialist on Laboratory Methods Author: Bc. Lenka Králíková Supervisor: PharmDr. Ondřej Janďourek, Ph.D. Title of diploma: Atypical mycobacteria as causative agents of human diseases The aim of this diploma thesis is to summarize the history of mycobacteria, their classification, epidemiology of nontuberculous infections, clinical significance, diagnosis, resistance, and treatment options. Within the epidemiology, the way of managing tuberculosis and non-tuberculous mycobacterioses is compared. Mycobacterioses are rare diseases, which incidence is gradually increasing with the increasing number of immunocompromised patients. Based on the spot of infection, we divide them into lymphadenitis, skin lesions, lung disease and disseminated infections. The most frequently isolated pathogens are Mycobacterium avium complex, Mycobacterium ulcerans, Mycobacterium abscessus, Mycobacterium marinum and Mycobacterium kansasii. The experimental part is devoted to the antimycobacterial activity of newly synthesized compounds, which could find application in the future in the treatment of tuberculosis and other mycobacterioses. Substance testing was performed on strains of the genus Mycobacterium...
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Effectiveness of disinfectants for hygienic hand disinfection against clinically important strains of enterococci
Malíková, Martina ; Janďourek, Ondřej (advisor) ; Konečná, Klára (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Study program: Bioanalytical laboratory diagnostics in health care Candidate: Bc. Martina Malíková Thesis supervisor: PharmDr. Ondřej Janďourek, Ph.D. Consultant: RNDr. Irena Hanovcová, CSc. Title of diploma thesis: Effectiveness of disinfectants for hygienic hand disinfection against clinically important strains of enterococci Alcohol-based hand disinfectants for hygienic hand disinfection are a key tool for the control of nosocomial infections worldwide. The aim of this study was to verify the effectiveness of these products, which are used in healthcare facilities, against vancomycin-sensitive and vancomycin-resistant enterococci isolated from clinical materials. Testing of the efficacy of disinfectants was performed according to the Czech technical standard ČSN EN 1040 - Chemical disinfectants and antiseptics - Quantitative test using suspension to determine the basic bactericidal effect of chemical disinfectants and antiseptics - Test method and requirements (phase 1). We used the dilution method with a neutraliser for our testing. There were used a total of 35 strains of enterococci to determine efficacy, 12 of which were vancomycin sensitive (four E. faecium strains and eight E. faecalis...
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Streptococcus agalactiae - antibiotic rezistence
Dvořáková, Andrea ; Voxová, Barbora (advisor) ; Janďourek, Ondřej (referee)
Streptococcus agalactie is an important pathogen causing very dangerous illnesses, especially in newborns. The aim of this work was to find out how resistant this microbe is to ATB (erythromycin, clindamycin, chloramphenicol, trimethoprim + sulfonamide, nitrofurantoin, penicillin, tetracycline, vancomycin and linezolid). At first testing was conducted on all watched group and subsequently on pregnant women and other patients. After the experimental stage, results from the pregnant women were compared with results from other tested group. In years 2018-2019, 1619 strains from 1295 patients in ÚKM FNHK were isolated. Sensitivity to ATB was measured in 1355 samples from 1105 patients. Within the all watched group of patients, resistance to each ATB was detected as follows: erythromycin (37,17 %), chloramphenicol (2,36 %), clindamycin (31,96 %), trimethoprim + sulfonamide (3,99 %), nitrofurantoin (1,11 %), peniciline (0,22 %), tetracycline (73,28 %) and to vancomycin and linezolid (0,00 %) of isolates. The resistance in pregnant women was detected as follows: erythromycin (26,36 %), chloramphenicol (2,33 %), clindamycin (22,87 %), trimethoprim + sulfonamide (3,49 %), nitrofurantoin (0,45 %), peniciline (0,39 %) and to tetracykcline (74,42 %) of isolates. After comparing results of resistance from...
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Mycobacterium tuberculosis as causative agent of grave illness
Hampl, Tomáš ; Janďourek, Ondřej (advisor) ; Voxová, Barbora (referee)
Charles University, Faculty of Pharmacy, Hradec Králové Field of study: Specialist in laboratory methods Author: Bc. Tomáš Hampl Supervisor: PharmDr. Ondřej Janďourek, Ph.D. Title of diploma thesis: Mycobacterium tuberculosis as causative agent of grave illness The aim of this diploma thesis is to deal with tuberculosis, describe the pathogen, taxonomic classification, describe the origin, course and clinical manifestations of the disease, diagnosis, including laboratory diagnostics, epidemiology of tuberculosis, treatment and prevention. Tuberculosis (TBC) is one of the deadliest infectious diseases in the world caused by bacterium M. tuberculosis in humans. TBC is sometimes referred as a disease of the past, but the recent rise in cases of the disease, and especially the spread of forms of drug-resistant TBC, makes the disease very dangerous. Currently, a major problem is the alarming rise in resistant and multi-resistant tuberculosis, which is not counteracted by commonly used first-line drugs. Therefore, there is a constant emphasis around the world on discovering and testing new potential antituberculotics that could help patients with resistant and multidrug-resistant TBC. In the experimental part, the thesis deals with screening of antimycobacterial activity of potential antituberculotics...
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