Anti-tubercular Drug Design Exploring Mycobactin Biosynthetic Pathway. Designing molecules that mimics hydroxyphenyl oxazoline portion of mycobactin

      Аннотация: “since a growth factor for Mycobacterium paratuberculosis was produced by Mycobacterium tuberculosis and seemed highly specific for the mycobacteria, its structure, if known, should provide a highly suitable model for the synthesis of compounds having a specific action against the mycobacteria” ..... Francis, J (1945) in Bacteriol Rev, 1970, 34, 99-125 by Snow, GA *****Small molecule heterocyclic compounds that mimics hydroxyphenyl oxazoline portion of mycobactin were designed to interfere mycobactin biosynthesis. Mycobactin is a mycobacterial "siderophore" responsible for iron acquisition from host cell. Iron and mycobactin are two important virulence factors and restricting the iron acquisition by blocking the mycobactin biosynthesis will in turn affect the growth of mycobacteria inside the host cell. A library of around thirty-nine molecules were synthesized and tested for their anti-tubercular activity under iron rich and deprived media. *****

Ключевые слова: antitubercular, Mycobactin analogues, Pyrazolines, Mycobacterium tuberculosis, Yersinia pestis