ArticleBioorganic & medicinal chemistry2013
Design, synthesis and characterization of novel 1,2-benzisothiazol-3(2H)-one and 1,3,4-oxadiazole hybrid derivatives: potent inhibitors of Dengue and West Nile virus NS2B/NS3 proteases.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 73 citations in OpenAlex.
- Achievements and Approaches in the Search for Small-Molecule Dengue NS2B/NS3 Inhibitors.Current medicinal chemistry · 2026Review
- Recent Advances in the Synthesis of Benzo[Molecules (Basel, Switzerland) · 2025Review
- Advances in antiviral strategies targeting mosquito-borne viruses: cellular, viral, and immune-related approaches.Virology journal · 2025Review
- Dengue virus: pathogenesis and potential for small molecule inhibitors.Bioscience reports · 2024Review
- Selective Oxidation of Benzo[Molecules (Basel, Switzerland) · 2024Article
- Article
- Development in the Inhibition of Dengue Proteases as Drug Targets.Current medicinal chemistry · 2024Review
- Review
- Targeting the protease of West Nile virus.RSC medicinal chemistry · 2021Review
- Facile Synthesis and In Vitro Activity ofPathogens (Basel, Switzerland) · 2021Article
- 1,3,4-OxadiazoleMolecules (Basel, Switzerland) · 2021Article
- Design and Synthesis of Small Molecules as PotentAntibiotics (Basel, Switzerland) · 2020Review
- Synthesis of new oxadiazol-phthalazinone derivatives with anti-proliferative activity; molecular docking, pro-apoptotic, and enzyme inhibition profile.RSC advances · 2020Article
- Co-cultivation ofFrontiers in microbiology · 2019Article
- Two New 1,3,4-Oxadiazoles With Effective Antifungal Activity AgainstFrontiers in microbiology · 2019Article
- Identification of novel small molecule inhibitors against NS2B/NS3 serine protease from Zika virus.Antiviral research · 2017Article
- An Overview of Current Approaches Toward the Treatment and Prevention of West Nile Virus Infection.Methods in molecular biology (Clifton, N.J.) · 2016Article
- 5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus.Journal of medicinal chemistry · 2015Article
- Identification of covalent active site inhibitors of dengue virus protease.Drug design, development and therapy · 2015Article
- The flavivirus protease as a target for drug discovery.Virologica Sinica · 2013Review
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
1,2-Benzisothiazol-3(2H)-ones and 1,3,4-oxadiazoles individually have recently attracted considerable interest in drug discovery, including as antibacterial and antifungal agents. In this study, a series of functionalized 1,2-benzisothiazol-3(2H)-one-1,3,4-oxadiazole hybrid derivatives were synthesized and subsequently screened against Dengue and West Nile virus proteases. Ten out of twenty-four compounds showed greater than 50% inhibition against DENV2 and WNV proteases ([I] = 10 μM). The IC(50) values of compound 7n against DENV2 and WNV NS2B/NS3 were found to be 3.75 ± 0.06 and 4.22 ± 0.07 μM, respectively. The kinetics data support a competitive mode of inhibition by compound 7n. Molecular modeling studies were performed to delineate the putative binding mode of this series of compounds. This study reveals that the hybrid series arising from the linking of the two scaffolds provides a suitable platform for conducting a hit-to-lead optimization campaign via iterative structure-activity relationship studies, in vitro screening and X-ray crystallography.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.