Antimycobacterial activity of 5-arylidene derivatives of hydantoin.
The synthesis of various 5-arylidene-2-thiohydantoins and results of the primary assay in vitro for their antimycobacterial activity is reported. Eight of those compounds exhibited > 90% inhibition of Mycobacterium tuberculosis growth and for them the minimum inhibitory concentrations, cytotoxicity (IC50) and the selectivity index values were determined. The most active structure, (5Z)-5-(1,1'-biphenyl-4-ylmethylene)-2-thioxoimidazolidin-4-one, showed MIC = 0.78 microg/ml. For all compounds log P and log D (pH 6.5) values were calculated.
Kieć-Kononowicz
K
K
Department of Chemical Technology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, ul Medyczna 9, PL 30-688 Kraków, Poland. mfkonono@kinga.cyf-kr.edu.pl
Szymańska
E
E
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002522:Chlorocebus aethiops; D004354:Drug Screening Assays, Antitumor; D006827:Hydantoins / Q000138:chemical synthesis* / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014709:Vero Cells
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D006827:Hydantoins; D007202:Indicators and Reagents