2. Academic Validation
  3. Design and synthesis of an N-benzyl 5-(4-sulfamoylbenzylidene-2-thioxothiazolidin-4-one scaffold as a novel NLRP3 inflammasome inhibitor

Design and synthesis of an N-benzyl 5-(4-sulfamoylbenzylidene-2-thioxothiazolidin-4-one scaffold as a novel NLRP3 inflammasome inhibitor

  • Bioorg Med Chem Lett. 2022 Jun 1;65:128693. doi: 10.1016/j.bmcl.2022.128693.
Dongxu Zuo 1,  Nayeon Do 1,  Inhwa Hwang 2,  Jihyae Ann 3,  Je-Wook Yu 4,  Jeewoo Lee 5
Affiliations

Affiliations

  • 1 Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
  • 2 Department of Microbiology and Immunology, BK 21 Project for Medical Science, Yonsei University College of Medicine, Seoul 03722, Republic of Korea.
  • 3 Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea. Electronic address: jihuya@snu.ac.kr.
  • 4 Department of Microbiology and Immunology, BK 21 Project for Medical Science, Yonsei University College of Medicine, Seoul 03722, Republic of Korea. Electronic address: jewookyu@yuhs.ac.
  • 5 Laboratory of Medicinal Chemistry, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea. Electronic address: jeewoo@snu.ac.kr.
PMID: 35314328 DOI: 10.1016/j.bmcl.2022.128693
Abstract

A series of N-benzyl 5-(4-sulfamoylbenzylidene-2-thioxothiazolidin-4-one analogs, designed as hybrids of CY09 and JC121, were investigated as inhibitors of NLRP3 inflammasome activation. Among them, compounds 34 and 36 were identified as promising NLRP3 inhibitors by measuring the amount of active Caspase-1 p20 and IL-1β produced by NLRP3 inflammasome activation. Further studies indicated that both compounds inhibited NLRP3 inflammasome assembly by reducing the formation of NLRP3 and ASC oligomer specks and selectively inhibited only NLRP3 inflammasome activation and not Other inflammasomes such as NLRC4 and AIM2.

Keywords

Inflammasome; Inhibitor; NLRP3; Neuroinflammation.

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