Identification of novel thiazole derivatives as flaviviral protease inhibitors effective against Dengue (DENV2) and Japanese encephalitis viruses.

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Tác giả: Sayan Das, Rikeshwer Prasad Dewangan, Indrani Das Jana, Venkatesan Jayaprakash, Arindam Mondal, Sheikh Murtuja, Gourav Rakshit, Biswatrish Sarkar, Deepak Shilkar, Barij Nayan Sinha

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : Antimicrobial agents and chemotherapy , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 676161

Flaviviruses are the causative agents of viral hemorrhagic fever (VHF) globally and have demonstrated the capacity to result in fatal outcomes if not managed effectively. Among different types of flaviviruses, dengue (DENV) and Japanese encephalitis (JEV) viruses are the most common in tropical and subtropical countries. While vaccines have been developed and licensed for both DENV and JEV, effective treatment options remain sparse. Hence, there is a pressing need to develop small molecules that can target machineries crucial for virus replication and remain conserved across different flaviviruses, thereby could serve as a promising therapeutic option. This study outlines the synthesis of novel thiazole compounds as flavivirus NS2B-NS3 protease inhibitor and characterization of their antiviral activity against DENV and JEV. We synthesized a heterocyclic template derived from a substrate-based retrotripeptide dengue protease inhibitor, leading to 48 thiazole derivatives. Two compounds, 3aq and 3au demonstrated significant inhibition of dengue virus protease activity
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