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Synthesis and molecular modelling studies of prenylated pyrazolines as MAO-B inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 20:6479-6482
- Publication Year :
- 2010
- Publisher :
- Elsevier BV, 2010.
-
Abstract
- A series of N-substituted-3-[(2′-hydroxy-4′-prenyloxy)-phenyl]-5-phenyl-4,5-dihydro-(1H)-pyrazolines were synthesized and tested on human monoamine oxidase-A and -B isoforms. Structure–activity relationships and molecular modelling showed that some substitutions, such as benzyloxy or chlorine atom, improve the best interaction with active site of hMAO-B.
- Subjects :
- Models, Molecular
Monoamine Oxidase Inhibitors
Stereochemistry
Clinical Biochemistry
Chlorine atom
Pharmaceutical Science
Biochemistry
Inhibitory Concentration 50
Structure-Activity Relationship
Prenylation
Drug Discovery
Humans
Monoamine Oxidase
Molecular Biology
Molecular Structure
biology
Chemistry
Organic Chemistry
Active site
Monoamine neurotransmitter
Docking (molecular)
biology.protein
Pyrazoles
Molecular Medicine
Monoamine oxidase B
5-dihydro-(1h)-pyrazole
docking
hmao-b inhibitors
prenylated pyrazoline
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 20
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....10a692515f69f79f007be700a3b8423b
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.09.061