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Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors
Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 13:1345-1348
- Publication Year :
- 2003
- Publisher :
- Elsevier BV, 2003.
-
Abstract
- Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme.
- Subjects :
- Clinical Biochemistry
Drug Evaluation, Preclinical
Pharmaceutical Science
Biochemistry
Chemical synthesis
IMPDH Inhibitors
Structure-Activity Relationship
chemistry.chemical_compound
IMP Dehydrogenase
IMP dehydrogenase
Drug Discovery
Escherichia coli
Humans
Potency
Enzyme Inhibitors
Isoquinoline
Oxazoles
Molecular Biology
chemistry.chemical_classification
biology
Chemistry
Organic Chemistry
Isoquinolines
NAD
In vitro
Enzyme
Enzyme inhibitor
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....53fc56fb4aaf95da3433bd20e11fd0d9
- Full Text :
- https://doi.org/10.1016/s0960-894x(03)00107-0