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• 作者：Sana Aslam (1) (2)
  Matloob Ahmad (3)
  Muhammad Makshoof Athar (2)
  Usman Ali Ashfaq (4)
  John M. Gardiner (5)
  Catherine Montero (6)
  Mervi Detorio (6)
  Masood Parvez (7)
  Raymond F. Schinazi (6)
  
• 关键词：Anti ; HIV ; 1 activity ; 1 ; 2 ; Benzothiazine ; Cytotoxic activity ; Hydrazides ; Pyrazolobenzothiazine dioxides
• 刊名：Medicinal Chemistry Research
• 出版年：2014
• 出版时间：June 2014
• 年：2014
• 卷：23
• 期：6
• 页码：2930-2946
• 全文大小：2,238 KB
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  2. Ahmad M, Siddiqui HL, Azam M, Bukhari IH, Parvez M (2010b) 2-(2-Oxo-2-phenylethyl)-1,2-benzisothiazol-3(2 / H)-one-1,1-dioxide. Acta Cryst E 66:o616 CrossRef
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  6. Ahmad M, Siddiqui HL, Gardiner JM, Parvez M, Aslam S (2013a) Synthesis and antioxidant studies of novel / N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3- / c][1,2]benzothiazin-2(4 / H)-yl)acetamides. Med Chem Res 22:794-05 CrossRef
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• 作者单位：Sana Aslam (1) (2)
  Matloob Ahmad (3)
  Muhammad Makshoof Athar (2)
  Usman Ali Ashfaq (4)
  John M. Gardiner (5)
  Catherine Montero (6)
  Mervi Detorio (6)
  Masood Parvez (7)
  Raymond F. Schinazi (6)
  
  1. Department of Chemistry, Government College Women University, Faisalabad, Pakistan
  2. Institute of Chemistry, University of the Punjab, Lahore, 54590, Pakistan
  3. Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan
  4. Department of Bioinformatics and Biotechnology, Government College University, Faisalabad, 38000, Pakistan
  5. School of Chemistry and Manchester Institute of Biotechnology, University of Manchester, Manchester, M1 7DN, UK
  6. Laboratory of Biochemical Pharmacology, Emory University School of Medicine/Veterans Affairs Medical Center, 1760 Haygood Drive, Atlanta, GA, 30322, USA
  7. Department of Chemistry, The University of Calgary, 2500 University Drive NW, Calgary, AB, T2N 1N4, Canada
  
• ISSN：1554-8120

文摘

N-Substitutedbenzylidene-2-(4-methyl-5,5-dioxido-3-phenylbenzo[e]pyrazolo[4,3-c][1,2]thiazin-1(4H)-yl)acetohydrazides (7a-strong class="a-plus-plus">u) were synthesized through a multistep reaction. The final compounds were screened for anti-HIV-1 and cytotoxic activities. Among these compounds, 7l and 7m exhibited the most significant anti-HIV-1 activity with EC50 values of 5.4 and 3.3?μM, respectively, while 7j showed moderate anti-HIV activity with an EC50 value 17.1?μM. Molecular docking into HIV-1 Reverse Transcriptase also showed the best fit for 7l and 7m followed by 7j. In addition, compounds 7b, 7f, 7h, 7k, 7o, and 7s exhibited no toxicity in all the three cell lines used i.e., primary human PBM, CEM, and Vero cells, while 7e, 7g, 7i, 7n, 7p, 7q, and 7t exhibited no cytotoxic activity in primary human PBM cells. Moreover, it was found through molecular docking that compounds 7l, 7m, and 7j bound efficiently in the NTP-binding pocket of HIV-1 Reverse Transcriptase. The structure–activity relationship established on these results would facilitate the further development of new HIV inhibitors based on this skeleton.