Patent number: 7345048
Abstract: The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and R4 and R4? are each independently hydrogen or a substituted or unsubstituted, linear, branched, or cyclic, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or hydrogen atoms may be substituted by a substituent selected from amino, alkylamino, hydroxyl, alkoxyl, thio, halogen, nitro, and carbonyl; wherein NR4R4? incorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NR4R4? is bonded to N through a substituted or unsubstituted alkylene moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway enzyme in bacterial cell-wall synthesis, and are suitable for various antibacterial uses.
Type:
Grant
Filed:
June 28, 2002
Date of Patent:
March 18, 2008
Assignee:
Pliva D.D.
Inventors:
Paul J. Ala, Janid A. Ali, Jacob J. Clement, Patrick R. Connelly, Carlos H. Faerman, Christopher Faraday, John V. Gazzaniga, Andrew S. Magee, Salvatore A. Marchese, Scott T. Moe, Manuel A. Navia, Emanuele Perola, Paul Will