Příprava derivátů pyrazinamidu jako potenciálních antiinfektiv. (Studium vztahů mezi chemickou strukturou a biologickou aktivitou)

Juhás, Martin

Charles University, Faculty of Pharmacy in Hradec Králové Training Workplace Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Doctoral Degree Program Pharmaceutical Chemistry Candidate PharmDr. Martin Juhás Supervisor doc. PharmDr. Jan Zitko, Ph.D. Advisor prof. PharmDr. Martin Doležal, Ph.D. Title of Doctoral Thesis Preparation of Pyrazinamide Derivatives as Potential Antiinfectives. (Study of Structure Activity Relationships) Antimicrobial resistance is considered one of the greatest threats of the 21st century. Until the COVID-19 pandemic, tuberculosis (TB) was the deadliest infectious disease, responsible for approx. one and a half million deaths each year. Resistance is very common in TB. Therefore, this work deals with the research of new potential antimicrobial substances with a particular focus on the activity against Mycobacterium tuberculosis, the main cause of TB. The introduction of this work briefly describes the current state of research on derivatives of pyrazinamide, which served as the prototype structure of the prepared substances and follows with a basic overview of modern computer-based methods used in drug design. The next part comments on the used chemical and biological methods, and the obtained structure-activity relationships in the presented publications....

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