N2-Benzyloxycarbonylguan-9-yl Acetic Acid Derivatives as HIV-1 Reverse Transcriptase Non-Nucleoside Inhibitors with Decreased Loss of Potency Against Common Drug-Resistance Mutations

N2-Benzyloxycarbonylguan-9-yl Acetic Acid Derivatives as HIV-1 Reverse Transcriptase Non-Nucleoside Inhibitors with Decreased Loss of Potency Against Common Drug-Resistance Mutations

Beating the RT mutants: A novel class of N2‐Cbz‐guan‐9‐yl acetic acid derivatives is endowed with anti‐HIV‐1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug‐resistant RT mutants relative to nevirapine and efavirenz. Their unique sc...

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Veröffentlicht in:ChemMedChem 2007-10, Vol.2 (10), p.1405-1409
Hauptverfasser: Adebambo, Kassim F., Zanoli, Samantha, Thomas, Michael G., Cancio, Reynel, Howarth, Nicola M., Maga, Giovanni
Format: Artikel
Sprache:eng
Schlagworte:
Acetates - chemistry
Acetates - pharmacology
antiviral agents
drug resistance
Drug Resistance, Viral - genetics
Guanine - analogs & derivatives
Guanine - chemistry
Guanine - pharmacology
HIV Reverse Transcriptase - antagonists & inhibitors
HIV-1 - drug effects
HIV-1 - genetics
Human immunodeficiency virus 1
kinetic analysis
Kinetics
NNRTIs
Reverse Transcriptase Inhibitors - chemistry
Reverse Transcriptase Inhibitors - pharmacology
slow binding
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Zusammenfassung:Beating the RT mutants: A novel class of N2‐Cbz‐guan‐9‐yl acetic acid derivatives is endowed with anti‐HIV‐1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug‐resistant RT mutants relative to nevirapine and efavirenz. Their unique scaffold and interesting resistance profiles warrant further development.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200700045