Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors
| Autor: | Qinghai Peng, Nowlin Dawn Marie, Hieu Lam, Ted William Johnson, Yang Anle, Wen Liu, Atsuo Kuki, Steven P. Tanis, Jon E. Kuehler, Zhang Junhu, Hai Wang, Plewe Michael Bruno, Scott L. Butler, Tran Khanh Tuan, Qiyue Hu, Sadayappan V. Rahavendran, Klaus Ruprecht Dress |
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| Rok vydání: | 2009 |
| Předmět: |
Stereochemistry
Drug Evaluation Preclinical Integrase inhibitor HIV Integrase Hydroxamic Acids Ligands Chemical synthesis Inhibitory Concentration 50 chemistry.chemical_compound Drug Discovery Magnesium HIV Integrase Inhibitors chemistry.chemical_classification Hydroxamic acid biology Chemistry virus diseases Nucleotidyltransferase Integrase Enzyme Biochemistry Viral replication Enzyme inhibitor Picolines HIV-1 biology.protein Molecular Medicine |
| Zdroj: | Journal of Medicinal Chemistry. 52:7211-7219 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Herein, we report the discovery of azaindole carboxylic acids and azaindole hydroxamic acids as potent inhibitors of the HIV-1 IN enzyme and their structure-activity relationships. Several 4-fluorobenzyl substituted azaindole hydroxamic acids showed potent antiviral activities in cell-based assays and offered a structurally simple scaffold for the development of novel HIV-1 IN inhibitors. |
| Databáze: | OpenAIRE |
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