Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication
| Autor: | A Paessens, U M Billhardt, Irvin Winkler, C Meichsner, M Rösner, R Bender, J P Kleim, G Riess |
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| Rok vydání: | 1993 |
| Předmět: |
Molecular Sequence Data
Mice Inbred Strains Biology medicine.disease_cause Virus Replication Antiviral Agents Virus chemistry.chemical_compound Mice Quinoxaline Quinoxalines medicine Animals Pharmacology (medical) Lymphocytes Cells Cultured Pharmacology chemistry.chemical_classification Mutation Acquired Immunodeficiency Syndrome Base Sequence RNA-Directed DNA Polymerase Virology Molecular biology Reverse transcriptase In vitro HIV Reverse Transcriptase Infectious Diseases Enzyme chemistry Viral replication Enzyme inhibitor biology.protein Mutagenesis Site-Directed Reverse Transcriptase Inhibitors Female Research Article |
| Zdroj: | Antimicrobial agents and chemotherapy. 37(8) |
| ISSN: | 0066-4804 |
| Popis: | S-2720 [6-chloro-3,3-dimethyl-4-(isopropenyloxycarbonyl)-3,4- dihydroquinoxalin-2(1H)-thione], a quinoxaline derivative, was found to be a very potent inhibitor of both human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) activity and HIV-1 replication in tissue culture. Like other nonnucleoside RT inhibitors, S-2720 does not affect the HIV-2 RT. A S-2720-resistant virus was selected and shown to possess a mutation within the RT-coding region that has not previously been described. Notably, this mutation gives rise to a dramatic decrease in enzyme activity. S-2720, therefore, belongs to a new class of RT inhibitors that bind differently to the RT than other known nonnucleoside RT inhibitors. As no toxic effects were observed with S-2720 in mice, these quinoxaline derivatives deserve further evaluation to prove their potency as possible therapeutic agents for HIV-1 infection. |
| Databáze: | OpenAIRE |
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