Literature DB >> 19269185

Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity.

Hongcai Li1, Chao Wang, Tino Sanchez, Yanmei Tan, Chunying Jiang, Nouri Neamati, Guisen Zhao.   

Abstract

HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed.

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Year:  2009        PMID: 19269185     DOI: 10.1016/j.bmc.2009.01.077

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

1.  Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.

Authors:  Christopher J Bungard; Peter D Williams; Jeanine E Ballard; David J Bennett; Christian Beaulieu; Carolyn Bahnck-Teets; Steve S Carroll; Ronald K Chang; David C Dubost; John F Fay; Tracy L Diamond; Thomas J Greshock; Li Hao; M Katharine Holloway; Peter J Felock; Jennifer J Gesell; Hua-Poo Su; Jesse J Manikowski; Daniel J McKay; Mike Miller; Xu Min; Carmela Molinaro; Oscar M Moradei; Philippe G Nantermet; Christian Nadeau; Rosa I Sanchez; Tummanapalli Satyanarayana; William D Shipe; Sanjay K Singh; Vouy Linh Truong; Sivalenka Vijayasaradhi; Catherine M Wiscount; Joseph P Vacca; Sheldon N Crane; John A McCauley
Journal:  ACS Med Chem Lett       Date:  2016-05-09       Impact factor: 4.345

2.  Classification and Design of HIV-1 Integrase Inhibitors Based on Machine Learning.

Authors:  Junlin Zhou; Juan Hao; Lianxin Peng; Huaichuan Duan; Qing Luo; Hailian Yan; Hua Wan; Yichen Hu; Li Liang; Zhenjian Xie; Wei Liu; Gang Zhao; Jianping Hu
Journal:  Comput Math Methods Med       Date:  2021-04-01       Impact factor: 2.238

  2 in total

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