Urea/thiourea derivatives of quinazolinone–lysine conjugates: Synthesis and structure–activity relationships of a new series of antimicrobials

Synthesis of a series of urea/thiourea/acetamide/sulphonamide derivatives of quinazolinones conjugated lysine has been reported. Structures of the products have been determined by standard spectroscopical studies. All the compounds have been screened for their antibacterial studies and structure–act...

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Veröffentlicht in:European journal of medicinal chemistry 2011-06, Vol.46 (6), p.2530-2540
Hauptverfasser: Suresha, G.P., Suhas, R., Kapfo, Wethroe, Channe Gowda, D.
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Sprache:eng
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Zusammenfassung:Synthesis of a series of urea/thiourea/acetamide/sulphonamide derivatives of quinazolinones conjugated lysine has been reported. Structures of the products have been determined by standard spectroscopical studies. All the compounds have been screened for their antibacterial studies and structure–activity relationship has been developed. The activity profile revealed that the compounds containing urea and thiourea functionalities along with fluoro group have exerted a highly potent activity. Thus, the title compounds represent a novel class of potent antimicrobial agents. [Display omitted] ► Quinazolinone-lysine conjugates and urea/thiourea/acetamide/sulphonamide derivatives. ► Several compounds exhibited highly potent antimicrobial activity. ► Urea/thiourea and F groups were found to be essential for potent results.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2011.03.041