2. Academic Validation
  3. Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2

Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2

  • Bioorg Med Chem Lett. 2021 Jan 1:31:127667. doi: 10.1016/j.bmcl.2020.127667.
Young Sup Shin 1,  Jun Young Lee 1,  Soojin Noh 1,  Yoonna Kwak 1,  Sangeun Jeon 2,  Sunoh Kwon 3,  Young-Hee Jin 4,  Min Seong Jang 5,  Seungtaek Kim 2,  Jong Hwan Song 1,  Hyoung Rae Kim 1,  Chul Min Park 1
Affiliations

Affiliations

  • 1 Center for Convergent Research of Emerging Virus Infection (CEVI), Korea Research Institute of Chemical Technology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, South Korea.
  • 2 Zoonotic Virus Laboratory, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 13488, South Korea.
  • 3 Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea.
  • 4 KM Application Center, Korea Institute of Oriental Medicine, Dong-gu, Daegu 41062, South Korea.
  • 5 Department of Non-Clinical Studies, Korea Institute of Toxicology, Yuseong-gu, Daejeon 34114, South Korea.
PMID: 33160024 DOI: 10.1016/j.bmcl.2020.127667
Abstract

Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) continues to spread worldwide, with 25 million confirmed cases and 800 thousand deaths. Effective treatments to target SARS-CoV-2 are urgently needed. In the present study, we have identified a class of cyclic sulfonamide derivatives as novel SARS-CoV-2 inhibitors. Compound 13c of the synthesized compounds exhibited robust inhibitory activity (IC50 = 0.88 μM) against SARS-CoV-2 without cytotoxicity (CC50 > 25 μM), with a selectivity index (SI) of 30.7. In addition, compound 13c exhibited high oral bioavailability (77%) and metabolic stability with good safety profiles in hERG and cytotoxicity studies. The present study identified that cyclic sulfonamide derivatives are a promising new template for the development of anti-SARS-CoV-2 agents.

Keywords

Coronavirus; Cyclic sulfonamide; Inhibitor; SARS-CoV-2; Structure activity relationship.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z