Details

Autor(en) / Beteiligte

• Clements, Joseph S.
• Islam, Rafique
• Sun, Baonan
• Tong, Fan
• Gross, Aaron D.
• Bloomquist, Jeffrey R.
• Carlier, Paul R.

Titel

N′-mono- and N, N′-diacyl derivatives of benzyl and arylhydrazines as contact insecticides against adult Anopheles gambiae

Ist Teil von

• Pesticide biochemistry and physiology, 2017-11, Vol.143, p.33-38

Ort / Verlag

United States: Elsevier Inc

Erscheinungsjahr

2017

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• New public health insecticides are urgently required to prevent the spread of vector-borne disease. With the goal of identifying new K+-channel-directed mosquitocides, analogs of the RH-5849 family of diacyl t-butylhydrazines were synthesized and tested for topical toxicity against adult Anopheles gambiae, the African vector of malaria. In total, 80N′-monoacyl and N, N′-diacyl derivatives of benzyl- and arylhydrazines were prepared. Three compounds (2bo, 2kb, 3ab) were identified that were more toxic than RH-5849 and RH-1266. The potencies of these compounds to block K+ currents in An. gambiae and human Kv2.1 channels were assessed to address their possible mechanism of mosquitocidal action. Selectivity for inhibition of An. gambiae Kv2.1 vs human Kv2.1 did not exceed 3-fold. Furthermore, no correlation was seen between the potency of insecticidal action and K+ channel blocking potency. These observations, combined with the minimal knockdown seen with 2bo near its LD50 value, suggests a mode of action outside of the nervous system. [Display omitted] •Acyl hydrazines were explored as contact insecticides for adult Anopheles gambiae.•Mono and diacyl arylhydrazines were more toxic than agricultural insecticide RH-1266.•No correlation between contact toxicity and K+ channel blockade potency was seen.