2. Academic Validation
  3. Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro

Synthesis of 10,10'-bis(trifluoromethyl) marinopyrrole A derivatives and evaluation of their antiviral activities in vitro

  • Eur J Med Chem. 2022 Aug 5:238:114436. doi: 10.1016/j.ejmech.2022.114436.
Yaxin Xiao 1,  Jingjing Yang 2,  Liangjing Zou 1,  Pingzhou Wu 1,  Wei Li 3,  Yunzheng Yan 3,  Yuexiang Li 3,  Song Li 2,  Hao Song 4,  Wu Zhong 5,  Yong Qin 6
Affiliations

Affiliations

  • 1 Key Laboratory of Drug-Targeting and Drug Delivery System of the Education, Ministry and Sichuan Province, and SichuaMn Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan Province, China.
  • 2 National Engineering Research Center for the Emergence Drugs, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, China; School of Pharmaceutical Sciences, Hainan University, Haikou, 570228, Hainan Province, China.
  • 3 National Engineering Research Center for the Emergence Drugs, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, China.
  • 4 Key Laboratory of Drug-Targeting and Drug Delivery System of the Education, Ministry and Sichuan Province, and SichuaMn Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan Province, China. Electronic address: songhao@scu.edu.cn.
  • 5 National Engineering Research Center for the Emergence Drugs, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, China. Electronic address: zhongwu@bmi.ac.cn.
  • 6 Key Laboratory of Drug-Targeting and Drug Delivery System of the Education, Ministry and Sichuan Province, and SichuaMn Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan Province, China. Electronic address: yongqin@scu.edu.cn.
PMID: 35598412 DOI: 10.1016/j.ejmech.2022.114436
Abstract

Flavivirus and Enterovirus can emerge unexpectedly in human populations and cause a spectrum of potentially severe diseases or even death. Since effective vaccine is currently unavailable against most of these deadly viruses, Antiviral chemical drugs remain in urgent need. To meet this unmet demand, we developed a series of 10,10'-bis(trifluoromethyl) marinopyrrole A derivates bearing various substituents at C5'-positions, which exhibited impressive in vitro activities against flaviviruses (ZIKV, DENV, YFV, JEV) and enteroviruses (EV71, CA6, CA16). The lead compound 10,10'-bis(trifluoromethyl) marinopyrrole A 3 was highly effective against enteroviruses EV71 and CA16 in cultured cells, but with low inhibitory activities against Flavivirus. Elaborately modified from compound 3, compounds 32 and 33 with sulfhydryl aliphatic chains were found as promising ZIKV and DENV inhibitor; pyrazine-containing compound 19 is a potent broad-spectrum Flavivirus inhibitor; thiophene compound 15 exhibited prominent selective inhibitory effect against JEV-SA14, YFV-17D, in addition to broad-spectrum Enterovirus inhibitory effect. These results thus suggest that the 5'-sulfhydryl derivates of 10,10'-bis(trifluoromethyl) marinopyrrole A may be promising lead compounds for the development of novel anti-flavivirus and anti-enterovirus drugs.

Keywords

Antiviral; Enterovirus; Flavivirus; Marinopyrrole A derivatives.

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