Selective Linear Peptides with Melanocortin-4 Receptor (MC4-R) Agonist Activity

Abstract

Peptides of formulae I, II and III that selectively activate melanocortin-4 (MC-4) receptor activity.

1 . A compound of the formula: 
       
         
           
           
               
               
           
         
         wherein 
         m is 0 or 1; 
         n is 0 or 1; 
         R 1  is an unsubstituted linear or branched alkyl having from 1 to 8 carbon atoms; linear or branched alkyl having from 1 to 8 carbon atoms mono-substituted by phenyl or carboxyl; unsubstituted phenyl; or phenyl mono-substituted by fluoro, chloro or linear or branched alkyl having from 1 to 4 carbon atoms; 
         X is 
       
       
         
           
           
               
               
           
         
       
       wherein R 2 , R 3  and R 4  are independently hydrogen or a linear or branched alkoxy having from 1 to 4 carbon atoms, wherein when R 3  is alkoxy, R 2  and R 4  are both hydrogen;
 R 9  is hydrogen, linear or branched alkyl having from 1 to 3 carbons, linear or branched alkoxy having from 1 to 3 carbons, or unsubstituted phenoxy; 
 R 11  is cyclohexyl, cycloheptyl, or a branched alkyl having from 3 to 8 carbon atoms; 
 R 6  is hydrogen or methyl; 
 R 7  is 
 
       
         
           
           
               
               
           
         
       
       and R 8  is hydrogen or methyl; or
 Y is 
 
       
         
           
           
               
               
           
         
       
       and R 8  is hydrogen.