Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors
| Autor: | George V. De Lucca |
|---|---|
| Rok vydání: | 1997 |
| Předmět: |
chemistry.chemical_classification
biology Chemistry Organic Chemistry Clinical Biochemistry Human immunodeficiency virus (HIV) Pharmaceutical Science medicine.disease_cause Biochemistry Chemical synthesis Combinatorial chemistry chemistry.chemical_compound Enzyme Enzyme inhibitor Drug Discovery medicine biology.protein Molecular Medicine HIV Protease Inhibitor Triphenylphosphine Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 7:495-500 |
| ISSN: | 0960-894X |
| Popis: | Imidazolidinones were synthesized from 7-membered ring cyclic ureas via a sequential series of novel ring contraction reactions proceeding first through the tetrahydropyrimidinones and finally to the 5-membered ring heterocycle. These imidazolidinones are shown to be excellent HIV-PR inhibitors. The most potent compound 20 having a Ki = 17 nM. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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