Synthesis of some novel phosphorylated and thiophosphorylated benzimidazoles and benzothiazoles and their evaluation for larvicidal potential to Aedes albopictus and Culex quinquefasciatus.

Bioorg Med Chem Lett

Discovery Center, Process Technology Development Division, Defence Research & Development Establishment, Jhansi Road, Gwalior 474002, MP, India. Electronic address:

Published: July 2014

AI Article Synopsis

  • A series of benzimidazole and benzothiazole compounds were synthesized and tested for their ability to kill mosquito larvae, specifically targeting Aedes albopictus and Culex quinquefasciatus.
  • Three compounds demonstrated significant effectiveness, with one compound (10e) achieving complete mortality in both mosquito species.
  • The toxicity levels of compound 10e were measured, showing an LC50 of 6.42 mg/L against Aedes albopictus and 7.01 mg/L against Culex quinquefasciatus over different time periods, with Temephos serving as a reference control.

Article Abstract

Series of benzimidazole and benzothiazole linked phosphoramidates and phosphoramidothioates (5a-j) and benzimidazole linked phenylphosphoramidates and phenylphosphoramidothioates (10a-e) were synthesized. The title compounds were preliminary screened for mosquito larvicidal properties against Aedes albopictus and Culex quinquefasciatus at different concentration from 40 to 5 mg/L. Among the screened compounds three compounds revealed potential larvicidal effects with 100% mortality in the order of 10e>5j>5e. Compound 10e was found to be the most toxic compound to Ae. albopictus and Cx. quinquefasciatus. The LC50 of 10e against Ae. albopictus was found to be 6.42 and 5.25 mg/L at 24 and 48 h, respectively, whereas it was 7.01 and 3.88 mg/L, respectively in Cx. quinquefasciatus. Temephos was used as positive control.

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http://dx.doi.org/10.1016/j.bmcl.2014.04.082DOI Listing

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