Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

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SEVER B., ALTINTOP M. D., ÖZDEMİR A., Tabanca N., Estep A. S., Becnel J. J., ...More

OPEN CHEMISTRY, vol.17, no.1, pp.288-294, 2019 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 17 Issue: 1
  • Publication Date: 2019
  • Doi Number: 10.1515/chem-2019-0027
  • Journal Name: OPEN CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.288-294
  • Keywords: mosquito control, Aedes aegypti, benzothiazole, piperidine, docking studies, STEROL CARRIER PROTEIN-2, AEDES-AEGYPTI, RESISTANCE, MECHANISMS, PESTICIDES, MUTATIONS
  • Anadolu University Affiliated: Yes


Aedes aegypti is associated with the transmission of numerous human and animal diseases, such as yellow fever, dengue fever, chikungunya, and more recently Zika virus. Emerging insecticide resistance has created a need to develop new mosquitocidal agents for effective control operations. A series of benzothiazole-piperidine derivatives (1-24) were investigated for their larvicidal and adulticidal effects on Ae. aegypti. It was observed that compounds 2, 4, 6, 7, 8, 11 and 13 showed notable larvicidal activity. Furthermore, compounds 6 and 10 showed promising adulticidal activity. Based on the mosquitocidal properties of these compounds, docking studies were also carried out in the active site of the AeSCP2 enzyme to explore any insights into further in vitro enzyme studies. Docking results indicated that all these active compounds showed reasonable interactions with critical residues in the active site of this enzyme. This outcome suggested that these compounds might show their larvicidal and adulticidal effects via the inhibition of AeSCP2. According to in vitro and in silico studies, compounds 2, 4, 6, 7, 8, 10, 11 and 13 stand out as candidates for further studies.