Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors
| Autor: | John S. Andrews, Subhash C. Annedi, Suman Rakhit, Shawn Maddaford, Jailall Ramnauth, Joanne Patman, Paul Renton, Namrta Bhardwaj |
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| Rok vydání: | 2007 |
| Předmět: |
Gene isoform
Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Nitric Oxide Synthase Type I Biochemistry Isozyme Chemical synthesis Nitric oxide Inhibitory Concentration 50 chemistry.chemical_compound Drug Discovery Animals Humans Benzothiazoles Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Chemistry Organic Chemistry In vitro Rats Isoenzymes Nitric oxide synthase Thiazoles Enzyme Models Chemical Enzyme inhibitor Drug Design biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:2540-2544 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2007.02.011 |
| Popis: | A series of substituted 2-aminobenzothiazole compounds have been synthesized and evaluated as nitric oxide synthase (NOS) inhibitors. Compound 14 shows activity in the nM range and is selective for the human neuronal NOS isoform. We have also evaluated the compounds against the rat NOS isoforms. For some of the compounds, there are significant differences in NOS inhibitory activities between the human and rat enzymes. For example, compound 10b has nM activity against the rat nNOS while low microM activity against the human nNOS. |
| Databáze: | OpenAIRE |
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