Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators
| Autor: | John Deadman, Eric Dale Jones, David Ian Rhodes, Changjiang Yu, Nick Vandegraaff, Jonathan Coates, Xinming Li, Xiao Feng, Giang Thanh Le, Lisa Jane Winfield, Long Lu, Neeranat Thienthong |
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| Rok vydání: | 2010 |
| Předmět: |
Azoles
Stereochemistry Isostere Clinical Biochemistry Pharmaceutical Science Integrase inhibitor HIV Integrase Biochemistry Chemical synthesis Bridged Bicyclo Compounds Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Structure–activity relationship HIV Integrase Inhibitors Thiazole Molecular Biology Chelating Agents Oxazole biology Bicyclic molecule Organic Chemistry Integrase chemistry Metals Drug Design HIV-1 biology.protein Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:5909-5912 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.07.081 |
| Popis: | Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported. |
| Databáze: | OpenAIRE |
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