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Molecules 2017, 22(2), 213;

Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives and Analogs Targeting the NLRP3 Inflammasome

State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 21 January 2016 / Accepted: 24 January 2017 / Published: 30 January 2017
(This article belongs to the Section Medicinal Chemistry)
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A series of benzo[d]imidazole analogues of thiabenzole were synthesized and their antiinflammatory activities toward NLRP3 (nucleotide‐binding domain leucine‐rich repeat containing protein family,pyrin domain‐containing 3,also known as cryopyrin or NALP3) inflammasome were evaluated in vitro. Two lead compounds, TBZ‐09 and TBZ‐21, were identified by antiproduction of IL‐1β. In the second round of biological evaluation, based on the lead, 34 more compounds were synthesized and their in vitro anti‐inflammatory activities were investigated. Several compounds were identified as anti‐inflammatory agents that can reduce IL‐1β expression in a dosedependent manner. A preliminary structure–activity relationship is also summarized here. View Full-Text
Keywords: benzimidazole; NLRP3; IL‐1β; anti‐inflammatory; drug discovery benzimidazole; NLRP3; IL‐1β; anti‐inflammatory; drug discovery

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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 (CC BY 4.0).

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Pan, L.; Hang, N.; Zhang, C.; Chen, Y.; Li, S.; Sun, Y.; Li, Z.; Meng, X. Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives and Analogs Targeting the NLRP3 Inflammasome. Molecules 2017, 22, 213.

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