2. Academic Validation
  3. Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator

Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator

  • ACS Med Chem Lett. 2020 Jan 9;11(2):166-171. doi: 10.1021/acsmedchemlett.9b00550.
Hyo Gyeong Na 1 2,  Ali Imran 1,  Kyuneun Kim 1 2,  Hong Sik Han 1 2,  Young Jin Lee 1 2,  Myung-Jin Kim 3,  Chang-Soo Yun 1,  Young-Sik Jung 1 2,  Joo-Youn Lee 4,  Soo Bong Han 1 2
Affiliations

Affiliations

  • 1 Bio and Drug Discovery Division, Korea Research Institute of Chemical Technology, PO Box 107, Daejeon 34114, Republic of Korea.
  • 2 Department of Medicinal Chemistry and Pharmacology, University of Science & Technology, Daejeon 34113, Republic of Korea.
  • 3 AM Sciences, C-912, SK V1 GL Metrocity, 128, Beobwon-ro, Songpa-gu, Seoul, 05854, Republic of Korea.
  • 4 Chemical Data-Driven Research Center, Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, Republic of Korea.
PMID: 32071684 DOI: 10.1021/acsmedchemlett.9b00550
Abstract

Hepatitis B virus (HBV) remains a major health concern with 260 million people having been infected globally, and approximately 680,000 deaths have occurred annually from cirrhosis and liver Cancer. The modulation of HBV capsid assembly has emerged as a promising therapeutic approach for curing chronic HBV Infection. Small-molecule capsid assembly modulators (CAMs) can broadly be classified as heteroaryldihydropyrimidines and sulfamoylbenzamides (SBAs). SBAs are capsid activators that inhibit viral replication by achieving capsid assembly before polymerase encapsulation. Herein, we report a novel series of HBV CAMs based on NVR 3-778, a potent CAM belonging to the SBA class. The lead compound (KR-26556) exhibited improved pharmacological activity and was examined through molecular docking studies.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-136111
    HBV衣壳组装调节剂
    HBV
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