title: Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors.
abstract: A series of novel 2,3-dihydro-1,3,4-oxadiazoles containing N-pyridylpyrazole carboxamides moieties were obtained by applying a new synthetic route. Their insecticidal tests against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of the compounds showed moderate to excellent activities at the testing concentrations. In particular, compound 6a showed 40% larvicidal activities against oriental armyworm at 1mg/L, while 7a against diamondback was 100% at 0.01mg/L. Calcium imaging results demonstrated that 6a, 6d and 7a stimulated a transient elevation in [Ca(2+)]i in the absence of external calcium after the central neurons dye loading with fluo-3 AM, implying that these novel compounds were potential activators of the ligand-gated calcium channel on the endoplasmic reticulum.
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Yunyun
authors.initials: Y
authors.lastname: Zhou
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Baolei
authors.initials: B
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Fengjuan
authors.initials: F
authors.lastname: Di
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Lixia
authors.initials: L
authors.lastname: Xiong
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Na
authors.initials: N
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
authors.forename: Yongqiang
authors.initials: Y
authors.lastname: Li
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China. Electronic address: liyx128@nankai.edu.cn.
authors.forename: Yuxin
authors.initials: Y
authors.lastname: Li
authors.affiliation: State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China. Electronic address: nkzml@vip.163.com.
authors.forename: Zhengming
authors.initials: Z
authors.lastname: Li
mesh_terms: D000818:Animals; D015195:Drug Design; D007306:Insecticides / Q000138:chemical synthesis / Q000494:pharmacology; D009036:Moths / Q000187:drug effects; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D019837:Ryanodine Receptor Calcium Release Channel / Q000737:chemistry / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D007306:Insecticides; D010069:Oxadiazoles; D019837:Ryanodine Receptor Calcium Release Channel; C583463:1,3,4-oxadiazole
keywords: 2,3-Dihydro-1,3,4-oxadiazoles; Calcium channel; Insecticidal activity