1.
Bioorg Med Chem Lett
; 18(23): 6100-3, 2008 Dec 01.
Article
in English
| MEDLINE
| ID: mdl-18947997
ABSTRACT
A successful scaffold-hopping approach gave a novel series of inhibitors of bacterial glutamate racemase (MurI). Early SAR studies of the 8-benzyl pteridine-6,7-diones led to compounds with micromolar enzyme potency and antibacterial activity.
Subject(s)
Amino Acid Isomerases/antagonists & inhibitors , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Gram-Positive Bacteria/enzymology , Pteridines/chemical synthesis , Pteridines/pharmacology , Anti-Bacterial Agents/chemistry , Combinatorial Chemistry Techniques , Gram-Positive Bacteria/drug effects , Microbial Sensitivity Tests , Molecular Structure , Pteridines/chemistry , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 18(15): 4368-72, 2008 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-18614367
ABSTRACT
An early SAR study of a screening hit series has generated a series of 9-benzyl purines as inhibitors of bacterial glutamate racemase (MurI) with micromolar enzyme potency and improved physical properties. X-ray co-crystal EI structures were obtained.