Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5′-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro

Xi-Wen Zeng; Ning Huang; Hui Xu; Wen-Bin Yang; Liu-Meng Yang; Huan Qu; Yong-Tang Zheng

doi:10.1248/cpb.58.976

Notes

Anti Human Immunodeficiency Virus Type 1 (HIV-1) Agents 4. Discovery of 5,5′-(p-Phenylenebisazo)-8-hydroxyquinoline Sulfonates as New HIV-1 Inhibitors in Vitro

Xi-Wen Zeng, Ning Huang, Hui Xu, Wen-Bin Yang, Liu-Meng Yang, Huan Qu, Yong-Tang Zheng

Author information

Xi-Wen Zeng
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University
Ning Huang
Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences
Hui Xu
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University
Wen-Bin Yang
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University
Liu-Meng Yang
Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences
Huan Qu
Laboratory of Pharmaceutical Design & Synthesis, College of Sciences, Northwest A&F University
Yong-Tang Zheng
Key Laboratory of Animal Models and Human Diseases Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences

Keywords: 8-hydroxyquinoline, sulfonate, acquired immune-deficiency syndrome, human immunodeficiency virus-1, inhibitor

JOURNAL FREE ACCESS

2010 Volume 58 Issue 7 Pages 976-979

DOI https://doi.org/10.1248/cpb.58.976

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Abstract

To search for compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, ten 5,5′-(p-phenylenebisazo)-8-hydroxyquinoline sulfonates (4a—j) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro for the first time. Some compounds demonstrated anti-HIV-1 activity, especially 5,5′-(p-phenylenebisazo)-8-hydroxyquinoline p-ethylbenzenesulfonate (4g) and 5,5′-(p-phenylenebisazo)-8-hydroxyquinoline p-chlorobenzenesulfonate (4i) showed the more potent anti-HIV-1 activity with 50% effective concentration (EC₅₀) values of 2.59 and 4.01 μg/ml, and therapeutic index (TI) values of 31.77 and 24.51, respectively.

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