Evidence map›Paper›PMID 29635166›Full record

ArticleEuropean journal of medicinal chemistry2018

Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.

Ye Tian, Zhaoqiang Liu, Jinghan Liu, Boshi Huang, Dongwei Kang, Heng Zhang, Erik De Clercq, Dirk Daelemans, Christophe Pannecouque, Kuo-Hsiung Lee and 3 more

Abstract read
In one paragraph

Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.

0numbers the graph read from it
0cells of the map it votes in
19citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

19 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
  5. Meldrum-Based-1ACS omega · 2023
    Article
  6. Novel Pyrano[3,2-ACS omega · 2023
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  7. Journal of medicinal chemistry · 2023
    Article
  8. Discovery of New Boswellic Acid Hybrid 1Pharmaceuticals (Basel, Switzerland) · 2023
    Article
  9. Article
  10. Lead/Drug Discovery from Natural Resources.Molecules (Basel, Switzerland) · 2022
    Review
  11. Article
  12. Article
  13. Review
  14. Article
  15. Review
  16. NewRSC advances · 2019
    Article
  17. Article
  18. Article
  19. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors.

Ye TianDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.
Zhaoqiang LiuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.
Jinghan LiuSchool of Life Science and Technology, China Pharmaceutical University, 639 Longmian Avenue, 210009, Nanjing, PR China.
Boshi HuangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.
Dongwei KangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.
Heng ZhangDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.
Erik De ClercqRega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
Dirk DaelemansRega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
Christophe PannecouqueRega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.
Kuo-Hsiung LeeNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599-7568, United States; Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan.
Chin-Ho ChenSurgical Science, Department of Surgery, Duke University Medical Center, Durham, NC, 27710, United States.
Peng ZhanDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China. Electronic address: zhanpeng1982@sdu.edu.cn.
Xinyong LiuDepartment of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China. Electronic address: xinyongl@sdu.edu.cn.

Funding

PLANT ANTIHIV AGENTSR01AI033066 · NIAID · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, KUO-HSIUNG · 1992 to 2018
$8.4M
NIAID NIH HHS R01 AI033066
6 · The paper itself

Abstract

Inspired by our previous efforts on the modifications of diarylpyrimidines as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTI) and reported crystallography study, novel diarylnicotinamide derivatives were designed with a "triazole tail" occupying the entrance channel in the NNRTI binding pocket of the reverse transcriptase to afford additional interactions. The newly designed compounds were then synthesized and evaluated for their anti-HIV activities in MT-4 cells. All the compounds showed excellent to good activity against wild-type HIV-1 strain with EC

Indexed as

Anti-HIV AgentsDrug DesignHIV-1HIV InfectionsHIV Reverse TranscriptaseHumansMolecular Docking SimulationNiacinamidePoint MutationStructure-Activity RelationshipTriazolesAnti-HIV AgentsHIV Reverse TranscriptaseNiacinamideTriazolesDiarylnicotinamideDrug designEntrance channelHIV-1NNRTIsTriazole

Identifiers

PMID29635166
PMCPMC6001364

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.