Bioorganic & Medicinal Chemistry Letters 28 (2018) 1149–1153 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Bioactivity and structure–activity relationship of cinnamic acid derivatives and its heteroaromatic ring analogues as potential high-efﬁcient acaricides against Psoroptes cuniculi a a ⇑ ⇑ Dong-Dong Chen , Bing-Yu Zhang , Xiu-Xiu Liu, Xing-Qiang Li, Xin-Juan Yang , Le Zhou College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi 712100, China article i nfo abstract Article history: A series of cinnamic acid derivatives and its heteroaromatic ring analogues were synthesized and Received 16 March 2017 evaluated for acaricidal activity in vitro against Psoroptes cuniculi, a mange mite. Among them, eight Revised 14 August 2017 compounds showed the higher activity with median lethal concentrations (LC ) of 0.36–1.07 mM Accepted 19 August 2017 (60.4–192.1 mg/mL) and great potential for the development of novel acaricidal agent. Compound 40 Available online 24 August 2017 showed both the lowest LC value of 0.36 mM (60.4 mg/mL) and the smallest median lethal time (LT ) of 2.6 h at 4.5 mM, comparable with ivermectin [LC = 0.28 mM (247.4 mg/mL), LT = 8.9 h], an 50 50 50 Keywords: acaricidal drug standard. SAR
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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