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Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation)
Vaňásková, Barbora ; Doležal, Martin (advisor) ; Zimčík, Petr (referee) ; Malík, Ivan (referee)
Charles University in Prague, Faculty of Pharmacy v Hradci Králové Department: Department of Pharmaceutical Chemistry and Drug Control Candidate: Mgr. Barbora Vaňásková Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation) This doctoral thesis deals with searching for potential antituberculotic drugs derived from pyrazinecarboxylic acid. Thesis contains theoretical part, in which problematics of tuberculosis, factors hindering the effectiveness of treatment (development of resistance and HIV coinfection) and current therapeutic practice are outlined. An individual chapter is devoted to the composition of the mycobacterial cell wall. A brief overview of first-line and second-line antituberculars as well as drugs newly introduced into the clinical practice and promising derivatives in various phases of preclinical and clinical trials is further stated. Special attention is dedicated to pyrazinamide, current theories dealing with mechanism of action of this first-line antituberculotic drug and to ribosomal protein S1, a specific target of pyrazinecarboxylic acid. A summary of pyrazinamide derivatives with antimycobacterial activity published since 2011 is listed for...
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Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation)
Vaňásková, Barbora ; Doležal, Martin (advisor) ; Zimčík, Petr (referee) ; Malík, Ivan (referee)
Charles University in Prague, Faculty of Pharmacy v Hradci Králové Department: Department of Pharmaceutical Chemistry and Drug Control Candidate: Mgr. Barbora Vaňásková Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation) This doctoral thesis deals with searching for potential antituberculotic drugs derived from pyrazinecarboxylic acid. Thesis contains theoretical part, in which problematics of tuberculosis, factors hindering the effectiveness of treatment (development of resistance and HIV coinfection) and current therapeutic practice are outlined. An individual chapter is devoted to the composition of the mycobacterial cell wall. A brief overview of first-line and second-line antituberculars as well as drugs newly introduced into the clinical practice and promising derivatives in various phases of preclinical and clinical trials is further stated. Special attention is dedicated to pyrazinamide, current theories dealing with mechanism of action of this first-line antituberculotic drug and to ribosomal protein S1, a specific target of pyrazinecarboxylic acid. A summary of pyrazinamide derivatives with antimycobacterial activity published since 2011 is listed for...
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Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation)
Vaňásková, Barbora ; Doležal, Martin (advisor) ; Zimčík, Petr (referee) ; Malík, Ivan (referee)
Charles University in Prague, Faculty of Pharmacy v Hradci Králové Department: Department of Pharmaceutical Chemistry and Drug Control Candidate: Mgr. Barbora Vaňásková Supervisor: Prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis: Derivatives of pyrazinecarboxylic acid as potential antituberculotics (synthesis and biological evaluation) This doctoral thesis deals with searching for potential antituberculotic drugs derived from pyrazinecarboxylic acid. Thesis contains theoretical part, in which problematics of tuberculosis, factors hindering the effectiveness of treatment (development of resistance and HIV coinfection) and current therapeutic practice are outlined. An individual chapter is devoted to the composition of the mycobacterial cell wall. A brief overview of first-line and second-line antituberculars as well as drugs newly introduced into the clinical practice and promising derivatives in various phases of preclinical and clinical trials is further stated. Special attention is dedicated to pyrazinamide, current theories dealing with mechanism of action of this first-line antituberculotic drug and to ribosomal protein S1, a specific target of pyrazinecarboxylic acid. A summary of pyrazinamide derivatives with antimycobacterial activity published since 2011 is listed for...
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