Next Article in Journal
Synthesis and Protective Effect of Scutellarein on Focal Cerebral Ischemia/Reperfusion in Rats
Previous Article in Journal
Advances in the Chemical Analysis and Biological Activities of Chuanxiong
Molecules 2012, 17(9), 10652-10666; doi:10.3390/molecules170910652
Article

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

1,* , 1, 1,2, 1, 1, 1 and 1
1 College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China 2 College of Chemical Engineering, Anhui University of Science Technology, Huainan 232001, China
* Author to whom correspondence should be addressed.
Received: 6 July 2012 / Revised: 6 August 2012 / Accepted: 24 August 2012 / Published: 6 September 2012
(This article belongs to the Section Medicinal Chemistry)
Download PDF [305 KB, uploaded 18 June 2014]

Abstract

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 1H-NMR, 13C-NMR and ESI (or HRMS) spectra. Detailed synthetic protocols and the anti-IN activity studies are also presented.
Keywords: HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives HIV-1; integrase inhibitors; quinolone-3-carboxylic acid derivatives
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Export to BibTeX |
EndNote


MDPI and ACS Style

Hu, L.; Yan, S.; Luo, Z.; Han, X.; Wang, Y.; Wang, Z.; Zeng, C. Design, Practical Synthesis, and Biological Evaluation of Novel 6-(Pyrazolylmethyl)-4-quinoline-3-carboxylic Acid Derivatives as HIV-1 Integrase Inhibitors. Molecules 2012, 17, 10652-10666.

View more citation formats

Related Articles

Article Metrics

Comments

Citing Articles

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert