Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors

A series of novel 6-(pyrazolylmethyl)-4-oxo-4H-quinoline-3-carboxylic acid derivatives bearing different substituents on the N-position of quinoline ring were designed and synthesized as potential HIV-1 integrase (IN) inhibitors, based on the structurally related GS-9137 scaffold. The structures of...

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Autores principales: Hu, Liming, Yan, Song, Luo, Zaigang, Han, Xiao, Wang, Yujie, Wang, Zhanyang, Zeng, Chengchu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268108/
https://www.ncbi.nlm.nih.gov/pubmed/22955454
http://dx.doi.org/10.3390/molecules170910652
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author Hu, Liming
Yan, Song
Luo, Zaigang
Han, Xiao
Wang, Yujie
Wang, Zhanyang
Zeng, Chengchu
author_facet Hu, Liming
Yan, Song
Luo, Zaigang
Han, Xiao
Wang, Yujie
Wang, Zhanyang
Zeng, Chengchu
author_sort Hu, Liming
collection PubMed
description A series of novel 6-(pyrazolylmethyl)-4-oxo-4H-quinoline-3-carboxylic acid derivatives bearing different substituents on the N-position of quinoline ring were designed and synthesized as potential HIV-1 integrase (IN) inhibitors, based on the structurally related GS-9137 scaffold. The structures of all new compounds were confirmed by (1)H-NMR, (13)C-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.
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spelling pubmed-62681082018-12-12 Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors Hu, Liming Yan, Song Luo, Zaigang Han, Xiao Wang, Yujie Wang, Zhanyang Zeng, Chengchu Molecules Article A series of novel 6-(pyrazolylmethyl)-4-oxo-4H-quinoline-3-carboxylic acid derivatives bearing different substituents on the N-position of quinoline ring were designed and synthesized as potential HIV-1 integrase (IN) inhibitors, based on the structurally related GS-9137 scaffold. The structures of all new compounds were confirmed by (1)H-NMR, (13)C-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented. MDPI 2012-09-06 /pmc/articles/PMC6268108/ /pubmed/22955454 http://dx.doi.org/10.3390/molecules170910652 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Hu, Liming
Yan, Song
Luo, Zaigang
Han, Xiao
Wang, Yujie
Wang, Zhanyang
Zeng, Chengchu
Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title_full Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title_fullStr Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title_full_unstemmed Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title_short Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors
title_sort design, practical synthesis, and biological evaluation of novel 6-(pyrazolylmethyl)-4-quinoline-3-carboxylic acid derivatives as hiv-1 integrase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268108/
https://www.ncbi.nlm.nih.gov/pubmed/22955454
http://dx.doi.org/10.3390/molecules170910652
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