Novel lactams

Abstract

The present invention relates to novel lactams of formulae (I) and (II). The present invention further relates to the use of these compounds in the treatment of microbial infections and microbial contamination of surfaces, particularly infections and surface contaminations characterised by biofilm formation. Further provided are compounds of formula (I) and (II) substituted with acrylate or methacrylate groups and their attachment to surfaces or polymers to inhibit microbial contamination.

1 - 20 . (canceled) 
     
     
         21 . A compound of formula I: 
       
         
           
           
               
               
           
         
         wherein: 
         R 1  is hydrogen; 
         R 2  is selected from the group consisting of heterocyclyl, heteroaryl, aryl and arylalkyl; 
         R 3  is selected from the group consisting of hydrogen, hydroxy, alkyl, cycloalkyl, alkoxy, oxoalkyl, alkenyl, heterocyclyl, heteroaryl, cycloalkyl, aryl, arylalkyl, and —C(O)CR 6 ═CH 2 ; 
         R 4  and R 5  are each hydrogen; 
         R 6  is selected from the group consisting of hydrogen or methyl. 
       
     
     
         22 . The compound of  claim 21 , wherein R 3  is selected from hydrogen, methyl and phenyl. 
     
     
         23 . The compound of  claim 21 , wherein R 2  is phenyl. 
     
     
         24 . The compound of  claim 21 , wherein R 2  is mono-substituted phenyl. 
     
     
         25 . A compound of formula II: 
       
         
           
           
               
               
           
         
         wherein 
         R 1  is hydrogen; 
         R 2  is mono-substituted phenyl; 
         R 3  is selected from the group consisting of hydrogen, hydroxy, alkyl, cycloalkyl, alkoxy, oxoalkyl, alkenyl, heterocyclyl, heteroaryl, cycloalkyl, aryl, arylalkyl, and —C(O)CR 6 ═CH 2 ; 
         R 4  and R 5  are each hydrogen; 
         R 6  is selected from the group consisting of hydrogen or methyl. 
         R 7  is hydrogen. 
       
     
     
         26 . The compound of  claim 25 , wherein R 3  is selected from hydrogen, methyl and phenyl. 
     
     
         27 . A method of treating a microbial infection in a subject, the method comprising administering a compound according to  claim 21  to the subject. 
     
     
         28 . A method according to  claim 27  wherein the infection is a bacterial infection. 
     
     
         29 . A method according to  claim 27  wherein the infection is characterised by biofilm formation. 
     
     
         30 . A method of inhibiting microbial contamination of a surface, the method comprising administering a compound according to  claim 21  to the surface.