Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors

Sekgota, Khethobole C; Majumder, Swarup; Isaacs, Michelle; Mnkandhla, Dumisani; Hoppe, Heinrich C; Khanye, Setshaba D; Kriel, Frederik H; Coates, Judy; Kaye, Perry T

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
Creator: Majumder, Swarup
Creator: Isaacs, Michelle
Creator: Mnkandhla, Dumisani
Creator: Hoppe, Heinrich C
Creator: Khanye, Setshaba D
Creator: Kriel, Frederik H
Creator: Coates, Judy
Creator: Kaye, Perry T
Date Issued: 2017
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
Format: pdf
Language: English
Relation: Bioorganic Chemistry
Relation: 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
Relation: 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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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

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