Pliva D.d.

Paul Will

Emanuele Perola

Manuel A Navia

Patrick Raymond Connelly

Salvatore Anthony Marchese

Andrew Magee

Scott T Moe

Carlos H Faerman

Jacob J Clement

Christopher Faraday

John V Gazzaniga

Paul J Ala

Janid A Ali

The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein Ris NH; Ris NH; Ris selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and Rand Rare 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 NRRincorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NRRis 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.

Heterocyclic compounds and uses thereof as D-alanyl-D-alanine ligase inhibitors

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Stoneham, MA, United States of America

Paul Will