- Title
- Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors
- Creator
- Sekgota, Khethobole C, Majumder, Swarup, Isaacs, Michelle, Mnkandhla, Dumisani, Hoppe, Heinrich C, Khanye, Setshaba D, Kriel, Frederik H, Coates, Judy, Kaye, Perry T
- Date
- 2017
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/66178
- Identifier
- vital:28913
- Identifier
- https://doi.org/10.1016/j.bioorg.2017.09.015
- Description
- publisher version
- Description
- 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.
- Format
- 7 pages, pdf
- Language
- English
- Relation
- Bioorganic Chemistry, Sekgota, Khethobole C., Majumder, Swarup, Isaacs, Michelle, Mnkandhla, Dumisani, Hoppe, Heinrich C., Khanye, Setshaba D., Kriel, Frederik H., Coates, Judy, Kaye, Perry T. (2017) Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors. Bioorganic Chemistry, v. 75. p. 310 – 316. SN - 0045-2068. https://doi.org/10.1016/j.bioorg.2017.09.015, Bioorganic Chemistry volume 75 number 310 316 December 2017 0045-2068
- Rights
- Elsevier B.V.
- Rights
- Use of this resource is governed by the terms and conditions of the Bioorganic Chemistry Open Access Options Statement (https://www.elsevier.com/journals/bioorganic-chemistry/0045-2068/open-access-options)
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Collections
Khanye, David Setshaba (Associate Prof)
Hoppe, Heinrich C (Prof)
Isaacs, Michelle (Mrs)
Kaye, Perry T (Distinguished Fellow Emeritus Professor)
RU Department of Chemistry
RU Department of Pharmacy
RU Department of Biochemistry, Microbiology and Bioinformatics
SDG 03. Good Health and Well-Being
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