- Novel Anthranilic Diamide Scaffolds Containing N-Substituted Phenylpyrazole as Potential Ryanodine Receptor Activators
-
To discover potent insecticides targeting ryanodine receptors (RyRs), a series of novel anthranilic diamides analogues (12a-12u) containing N-substituted phenylpyrazole were designed and synthesized. These compounds were characterized by 1H NMR, 13C NMR, and HRMS, and the structure of compound 12u was confirmed by X-ray diffraction. Their insecticidal activities indicated that these compounds displayed moderate to excellent activities. In particular, 12i showed 100 and 37% larvicidal activities against oriental armyworm (Mythimna separata) at 0.25 and 0.05 mg L-1, equivalent to that of chlorantraniliprole (100%, 0.25 mg L-1; and 33%, 0.05 mg L-1). The activity of 12i against diamondback moth (Plutella xylostella) was 95% at 0.05 mg L-1, whereas the control was 100% at 0.05 mg L-1. The calcium-imaging technique experiment results showed that the effects of 12i on the intracellular calcium ion concentration ([Ca2+]i) in neurons were concentration-dependent. After the central neurons of Helicoverpa armigera were dyed by loading with fluo-5N and treated with 12i, the free calcium released in endoplasmic reticulum indicated the target of compound 12i is RyRs or IP3Rs. The activation of RyRs by natural ryanodine completely blocked the calcium release induced by 12i, which indicated that RyRs in the central neurons of H. armigera third-instar larvae is the possible target of compound 12i.
- Liu, Jing-Bo,Li, Yu-Xin,Zhang, Xiu-Lan,Hua, Xue-Wen,Wu, Chang-Chun,Wei, Wei,Wan, Ying-Ying,Cheng, Dan-Dan,Xiong, Li-Xia,Yang, Na,Song, Hai-Bin,Li, Zheng-Ming
-
p. 3697 - 3704
(2016/06/01)
-
- SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
-
The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
- -
-
-
- PROTEIN KINASE C INHIBITORS AND USES THEREOF
-
This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
- -
-
-
- Efficient and selective room-temperature gold-catalyzed reduction of nitro compounds with CO and H2O as the hydrogen source
-
[Chemical equation presented] Taking hydrogen from water: Gold catalysis enabled the selective reduction of nitro compounds under very mild conditions with a combination of H2O and CO as the reductant (see scheme). This environmentally friendly reaction proceeded in high yield and with high chemoselectivity in the presence of a wide range of functional groups
- He, Lin,Wang, Lu-Cun,Sun, Hao,Ni, Ji,Cao, Yong,He, Yong,Fan, Kang-Nian
-
supporting information; experimental part
p. 9538 - 9541
(2010/03/24)
-
- Small molecules useful in the treatment of inflammatory disease
-
Novel compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 5-(R)-(4-bromobenzyl)-3-(3-chloro-5-nitrophenyl)-5-methylimidazoline-2,4-dione; and, 5-(R)-(4-bromobenzyl
- -
-
Page column 28
(2010/02/05)
-