Patent ID: 7078380

Claim:
An antibacterial compound of formula V-L-W-X; wherein: V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria; L is a linking group; W is a peptidic membrane-associating element and is either a membrane binding peptide including at least one sequence (Xaa) n , where n is from 1 to 12 and each Xaa is independently lysine or arginine, and having an overall positive charge; or a membrane-inserting peptide; X is a membrane-insertive element and is a lipophilic chain wherein the lipophilic chain is described as: having from 6 to 30 carbon atoms including those of any aromatic rings; straight or branched containing one to three branch points; saturated or unsaturated containing one to four double or triple bonds; optionally having 1, 2 or 3 heteroatoms (in addition to those in any aromatic rings) independently selected from the group consisting of S, O and N; optionally containing one or more aromatic rings, which may be fused and each of which may contain from 1, 2 or 3 heteroatoms independently selected from the group consisting of N, O and S; and optionally having from one to three substituents selected from the group consisting of hydroxy, -SH, amino and halo; and V-L- is of the formula: wherein: Y and Y′ are independently hydrogen or chloro; R is selected from the group consisting of hydrogen, 4-epi-vancosaminyl, actinosaminyl, and ristosaminyl, or R is a group of the formula —R a -L- wherein R a is selected from the group consisting of 4-epi-vancosaminyl, actinosaminyl, and ristosaminyl and L is attached to the amino group of R a ; R 1 is hydrogen or mannose; R 2 is selected from the group consisting of —NH 2 , —NHCH 3 , —N(CH 3 ) 2 , —NHL-, and —N(CH 3 )L-; R 3 is selected from the group consisting of —CH 2 CH(CH 3 ) 2 , [p-OH, m-Cl]phenyl, p-rhamnose-phenyl, [p-rhamnose-galactose]phenyl, [p-galactose-galactose]phenyl, and [p-CH 3 O-rhamnose]phenyl; R 4 is selected from the group consisting of —CH 2 —(CO)NH 2 , benzyl, [p-OH]phenyl, and [p-OH, m-Cl]phenyl; R 5 is hydrogen or mannose, R 6 is selected from the group consisting of hydrogen, 4-epi-vancosaminyl, vancosaminyl, actinosaminyl, ristosaminyl, or acosaminyl; or R 6 is a group of the formula R b -L- wherein R b is selected from the group consisting of 4-epi-vancosaminyl, vancosaminyl, actinosaminyl, ristosaminyl and acosaminyl and L is attached to the amino group of R b ; or R 6 is a group R b —R 7 wherein R b is selected from the group consisting of 4-epi-vancosaminyl, vancosaminyl, actinosaminyl, ristosaminyl and acosaminyl and R 7 is an organic side chain moiety which is no more than 1000 Da; and Ter1 is hydroxy or -L-, provided that the compound includes at least one group -L-.