Bioorganic chemistry, 2017-12, Vol.75, p.310-316
2017
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Details
- Autor(en) / Beteiligte
- Titel
- Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors
- Ist Teil von
- Bioorganic chemistry, 2017-12, Vol.75, p.310-316
- Ort / Verlag
- United States: Elsevier Inc
- Erscheinungsjahr
- 2017
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- [Display omitted] •Novel application of Morita-Baylis-Hillman methodology in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones.•Selective in vitro inhibition of HIV-1 Integrase.•Low toxicity against HEK 293. A practicable six-step synthetic pathway has been developed to access a library of novel 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones using Morita-Baylis-Hillman methodology. These compounds and their 3-[(N-cycloalkylamino)methyl]-2-quinolone precursors have been screened as potential HIV-1 integrase (IN) inhibitors. A concomitant survey of their activity against HIV-1 protease and reverse-transcriptase reveals selective inhibition of HIV-1 IN.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0045-2068eISSN: 1090-2120DOI: 10.1016/j.bioorg.2017.09.015Titel-ID: cdi_proquest_miscellaneous_1957492243
- Format
- –
- Schlagworte
- 2-quinolones, Bioassay, Cell Survival - drug effects, Enzyme Activation - drug effects, HEK293 Cells, HIV Integrase - chemistry, HIV Integrase - metabolism, HIV Integrase Inhibitors - chemical synthesis, HIV Integrase Inhibitors - metabolism, HIV Integrase Inhibitors - pharmacology, HIV Reverse Transcriptase - antagonists & inhibitors, HIV Reverse Transcriptase - metabolism, HIV-1 - enzymology, HIV-1 integrase inhibitors, Humans, Morita_Baylis-Hillman, Quinolones - chemistry, Quinolones - metabolism, Quinolones - pharmacology, Structure-Activity Relationship, Synthesis