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Antibacterial Activity of Novel Sulfonylureas, Ureas and Thioureas of 15-Membered Azalides

The coupling of a arylsulfonyl and benzenesulfonamido moiety to the 9a position of 15-membered azalide scaffold via carbamoyl linker has indicated improvement in antibacterial activity of novel azalides. Hence, newly synthesised sulfonyl ureas of azalides 3b-3f, and azalide-sulfonamide conjugates 10a and 10b displayed significantly improved activity against inducible resistant S. pyogenes strain when compared to azithromycin. In addition, the introduction of carbamoyl and thiocarbamoyl group at the 9a position of azithromycin like azalide skeleton via propyl linker proved to be promising method to tackle the resistance problems. As a result of a preliminary optimization of an alkyl/aryl moiety attached at the carbamoyl and thiocarbamoyl group all prepared and tested compounds had high in vitro activity against erythromycin susceptible Gram-positive aerobes and Gram-negative microorganisms and especially resistant S. pyogenes and S. pneumoniae strains. It was also, shown here that urea and thiourea derivatives of 3-decladinosyl-3-hydroxy azalides, although lacking a cladinose sugar, showed noticeable antibacterial activity.

15-Membered azalides ; azalide-sulfonamide conjugates ; sulfonylureas ; ureas ; thioureas ; antibacterial activity

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