Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3404-3406
2011
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3404-3406
- Ort / Verlag
- Amsterdam: Elsevier Ltd
- Erscheinungsjahr
- 2011
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Novel heteroarylalanines derived from l-aspartic acid were designed and synthesised as potential inhibitors of Neutral Endopeptidase (NEP). Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2′ subsite within NEP. Structural optimisation led to the identification of 5-phenyl oxazole 4f, a potent and selective NEP inhibitor. A crystal structure of the inhibitor bound complex is reported.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2011.03.109Titel-ID: cdi_proquest_miscellaneous_872143015
- Format
- –
- Schlagworte
- Acids - chemical synthesis, Acids - chemistry, Acids - pharmacology, Alanine - chemical synthesis, Alanine - chemistry, Alanine - pharmacology, Angiotensin converting enzyme, Biological and medical sciences, Cardiovascular system, crystal structure, Crystallography, X-Ray, Enzyme Activation - drug effects, Humans, Inhibitory Concentration 50, Medical sciences, metalloproteinases, Miscellaneous, Models, Molecular, Molecular Structure, Neprilysin - antagonists & inhibitors, Neutral endopeptidase, Oxadiazole, Oxazole, oxazoles, Oxazoles - chemistry, Oxazoles - pharmacology, Pharmacology. Drug treatments, Protease Inhibitors - chemical synthesis, Protease Inhibitors - chemistry, Protease Inhibitors - pharmacology, zinc, Zinc metalloproteinases