Amino acid and peptide esters of abacavir: synthesis and activity against human immunodeficiency virus type 1 in cell culture
| Autor: | Radka Argirova, Petya D. Genova-Kalou, Ivanka Stankova, Ivailo I. Alexiev, Radoslav Chayrov, Anton Hinkov, Kamelia R. Stanoeva |
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| Rok vydání: | 2011 |
| Předmět: |
chemistry.chemical_classification
Anti-HIV activity Dipeptide Mitochondrial toxicity Organic Chemistry Peptide medicine.disease Amino acid chemistry.chemical_compound Aminoacid and dipeptide esters of abacavir chemistry Biochemistry Abacavir Cell culture Glycine Toxicity medicine Sequencing of HIV-mutants General Pharmacology Toxicology and Pharmaceutics medicine.drug |
| Zdroj: | Medicinal Chemistry Research. 21:4053-4059 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-011-9956-y |
| Popis: | Abacavir (ABC) is clinically associated with hypersensitivity reactions, risk for cardiovascular disease, etc. A possible way to minimize side effects is by modifying chemical structure. Three esters of ABC containing amino acid (glycine) and dipeptide esters (glycyl-glycine) were synthesized and their activity on HIV-1 III B replication in MT-4 cells was evaluated. One of the newly synthesized esters—Gly-ABC—demonstrates low-cytotoxicity and high-anti-HIV-1 activity in MT-4 cells, as well as low-mitochondrial toxicity and high-genetic barrier to resistance. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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