A new modification of anti-tubercular active molecules.
The connection of two active molecules across an easily released bridge as a new type of potentially active molecule has been studied. The synthesis is based on derivatives that originate from isonicotinoyl hydrazide, pyrazinamide, p-aminosalicylic acid (PAS), ethambutol, and ciprofloxacin. The lipophilicity, hydrolysis (stability of the compounds), and antituberculotic activity as well as the structure-lipophilicity and structure-activity relationships are discussed.
Imramovský
Ales
A
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 50005 Hradec Králové, Czech Republic. imramovsky@faf.cuni.cz
Polanc
Slovenko
S
Vinsová
Jarmila
J
Kocevar
Marijan
M
Jampílek
Josef
J
Recková
Zuzana
Z
Kaustová
Jarmila
J
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D007538:Isoniazid / Q000138:chemical synthesis / Q000494:pharmacology; D007700:Kinetics; D008055:Lipids / Q000737:chemistry; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects; D019909:Mycobacterium kansasii / Q000187:drug effects; D011718:Pyrazinamide / Q000138:chemical synthesis / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship
D000995:Antitubercular Agents; D008055:Lipids; D011718:Pyrazinamide; D007538:Isoniazid