申请人:Wadman Sjoerd Nicolaas
公开号:US20100261638A1
公开(公告)日:2010-10-14
The present invention provides actagardine, actagradine B and deoxy actagardine B derivatives of formula (I),
wherein: X1 denotes that the residue is Leu; Val; or Ile; X2 denotes that the residue is Leu; Val; or Ile; R
1
represents an alkyl or heteroalkyl group, substituted by at least one hydroxyl substituent, and R
2
represents hydrogen, or an alkyl or heteroalkyl group, optionally substituted by at least one hydroxyl substituent, or R
1
and R
2
taken together with the nitrogen atom represent a heterocyclic group having at least one hydroxyl substituent, wherein the heterocyclic group optionally further contains one or more heteroatoms; Z is an amino acid residue, —NR
3
R
4
, —NR
5
COR
6
, —NR
5
C(O)OR
6
; —NR
5
SOR
6
, NR
5
SO
2
R
6
; —NR
5
C(S)NR
6
R
7
, —NR
5
C(NR
8
)NR
6
R
7
, or —N═R
9
, where R
3
, R
4
, R
5
, R
6
, R
7
, R
8
and R
9
are independently hydrogen, or a group, optionally substituted, selected from alkyl, heteroalkyl, aryl, heteroaryl, aralkyl and heteroaralkyl, with the proviso that R
9
is not hydrogen; and Y is —S— or —S(O)—. The compounds find use in the treatment of microbial infections.