Macrocyclic inhibitors of the bacterial cell wall biosynthesis enzyme MurD.
Computer-based molecular design has been used to produce a series of new macrocyclic systems targeted against the bacterial cell wall biosynthetic enzyme MurD. Following their preparation, which involved a novel metathesis-based cyclisation as the key step, these systems were found to show good inhibition when assayed against the MurD enzyme.
Horton
James R
JR
Departments of Chemistry, University of Leeds, Leeds LS2 9JT, UK.
Bostock
Julieanne M
JM
Chopra
Ian
I
Hesse
Lars
L
Phillips
Simon E V
SE
Adams
David J
DJ
Johnson
A Peter
AP
Fishwick
Colin W G
CW
D001665:Binding Sites; D002473:Cell Wall / Q000737:chemistry / Q000378:metabolism; D017076:Computer-Aided Design; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D004926:Escherichia coli / Q000737:chemistry*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D008958:Models, Molecular; D010453:Peptide Synthases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D010453:Peptide Synthases; C053379:UDP-N-acetylmuramoylalanine-D-glutamate ligase