97928-01-3Relevant academic research and scientific papers
Discovery of evodiamine derivatives as potent insecticide candidates
Liu, Jingbo,Shi, Yabing,Chen, Shuting,Li, Fengyun,Wen, Wen,Wang, Yuanhong
, (2022/04/03)
In the search for novel more effective insecticides, natural products could be used as ideal template compounds due to their good environmental compatibility, various bioactivities, unique scaffolds and mode of action. We have found that natural product evodiamine, the main active component from the fruits of Evodia rutaecarpa (Juss.) Benth, displayed obvious insecticidal activities against lepidoptera pests. To continue our research, a series of evodiamine derivatives 3a-3aa were rationally designed and synthesized. The larvicidal activities results indicated that most of target compounds displayed better efficacy than evodiamine, matrine, and rotenone against Mythimna separata, Plutella xylostella and Helicoverpa armigera, among which 3z exhibited excellent larvicidal activities (65% at 2.5 mg/L against M. separata, 75% at 1.0 mg/L against P. xylostella, and 85% 10 mg/L against H. armigera, respectively), much better than evodiamine (0%), matrine (0%), and rotenone (0%). The preliminary structure activity relationships demonstrated that the fluorine atom at the E ring of evodiamine had a positive influence on the larvicidal activity. The calcium imaging experiment studies indicated that 3z could act on the ryanodine receptor (RyR) of M. separata and was an effective calcium activator for RyR.
New spiro pyrrole[2, 1-b]quinazolone derivative, preparation method and application thereof
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Paragraph 0132-0134, (2020/11/09)
The invention relates to a new spiro pyrrole[2, 1-b]quinazolone derivative, a preparation method and application thereof. The new spiro pyrrole[2, 1-b]quinazolone derivative is synthesized by using asimple method. The yield is high, the production cost is
Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one containing 4,5-dihydrothiazole-2-thiol derivatives against Meloidogyne incognita
Chen, Xiulei,Zhou, Zhen,Li, Zhong,Xu, Xiaoyong
, p. 194 - 200 (2019/09/13)
A series of novel 1,2,3-benzotriazin-4-one derivatives containing 4,5-dihydrothiazole-2-thiol were synthesized and characterized by 1H NMR, 13C NMR, 19F NMR and HRMS. The bioassay results showed that compounds 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-7-methoxybenzo[d][1–3]triazin-4(3H)-one, 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-6-nitrobenzo[d][1–3]triazin-4(3H)-one, 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1–3]triazin-4(3H)-one exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita at the concentration of 10.0 mg L?1 in vivo. Compound 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1–3]triazin-4(3H)-one showed excellent nematicidal activity with inhibition 68.3% at a concentration of 1.0 mg L?1. It suggested that the structure of 1,2,3-benzotriazin-4-one containing 4,5-dihydro-thiazole-2-thiol could be optimized further.
HARMFUL ARTHROPOD CONTROL METHOD USING HETEROCYCLIC COMPOUND
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Paragraph 0291, (2021/02/02)
PROBLEM TO BE SOLVED: To provide a method for controlling a harmful arthropod. SOLUTION: The compound shown by the formula (I) [in the formula, Q represents the group, etc. represented by the formula Q1, Z represents an oxygen atom, etc., A1 re
A phosgene and peroxide-free one-pot tandem synthesis of isatoic anhydrides involving anthranilic acid, boc anhydride and 2-chloro-N-methyl pyridinium iodide
Verma, Chhaya,Sharma, Somesh,Pathak, Arunendra
supporting information, p. 6897 - 6899 (2019/04/10)
A phosgene and peroxide-free approach for the synthesis of isatoic anhydrides has been described. The synthesis involves the carbamate formation with boc anhydride followed by in situ cyclization to afford the isatoic anhydride. The importance of this synthetic strategy is in the ease of operation, scalability and preparation from readily available raw materials.
The use of biochemical and biophysical tools for triage of high-throughput screening hits - aa case study with escherichia coli phosphopantetheine adenylyltransferase
Miller, J. Richard,Thanabal, Venkataraman,Melnick, Michael M.,Lall, Manjinder,Donovan, Charles,Sarver, Ronald W.,Lee, Doh-Yeel,Ohren, Jeff,Emerson, Don
scheme or table, p. 444 - 454 (2011/02/21)
High-throughput screening is utilized by pharmaceutical researchers and, increasingly, academic investigators to identify agents that act upon enzymes, receptors, and cellular processes. Screening hits include molecules that specifically bind the target and a greater number of non-specific compounds. It is necessary to 'triage' these hits to identify the subset worthy of further exploration. As part of our antibacterial drug discovery effort, we applied a suite of biochemical and biophysical tools to accelerate the triage process. We describe application of these tools to a series of 9-oxo-4,9-dihydropyrazolo[5, 1-b]quinazoline-2-carboxylic acids (PQ) hits from a screen of Escherichia coli phosphopantetheine adenylyltransferase (PPAT). Initial confirmation of specific binding to phosphopantetheine adenylyltransferase was obtained using biochemical and biophysical tools, including a novel orthogonal assay, isothermal titration calorimetry, and saturation transfer difference NMR. To identify the phosphopantetheine adenylyltransferase sub-site bound by these inhibitors, two techniques were utilized: steady-state enzyme kinetics and a novel 19F NMR method in which fluorine-containing fragments that bind the ATP and/or phosphopantetheine sites serve as competitive reporter probes. These data are consistent with PQs binding the ATP sub-site. In addition to identification of a series of PPAT inhibitors, the described hit triage process is broadly applicable to other enzyme targets in which milligram quantities of purified target protein are available.
PROLYL HYDROXYLASE ANTAGONISTS
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Page/Page column 93, (2010/11/26)
This invention relates to certain 2-[(quinolin-3-yl)carbonyl]aminoacetic acid derivatives of formula (I), where the various groups are defined herein, and which are useful in treating anemia.
Synthesis and pharmacological studies at the Gly/NMDA, AMPA and Kainate receptors of new oxazolo[4,5-c]quinolin-4-one derivatives bearing different substituents at position-2 and on the fused benzo ring
Calabri, Francesca Romana,Colotta, Vittoria,Catarzi, Daniela,Varano, Flavia,Lenzi, Ombretta,Filacchioni, Guido,Costagli, Chiara,Galli, Alessandro
, p. 897 - 907 (2007/10/03)
The synthesis and biological evaluation at the Gly/NMDA, AMPA and Kainate receptors of new oxazolo[4,5-c]quinolin-4-one derivatives are reported. Different substituents were introduced at the 2-position (mercapto, carbonyl and methyl groups) and on the fu
Antihypertensive 3-tetrazoyl-4-quinolones
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, (2008/06/13)
Novel quinolones of formula I STR1 and pharmaceutically acceptable acid addition salts thereof in which the dotted line between positions 2 and 3 of the quinolone ring represents an optional bond, R is hydrogen, 1-methyl or 2-lower alkyl; R1 is lower alkyl; R2 is hydrogen, halo, lower alkyl, lower alkoxy, trifluoromethyl, cyano, difluoromethoxy, methylsulphinyl, phenylsulphinyl or the group --NR4 R5 or the N-oxide thereof wherein R4 and R5, which may be the same or different, are lower alkyl or, together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino or morpholino radical; and R3 is hydrogen, fluoro, lower alkyl or lower alkoxy provided that, when R3 is lower alkoxy, R2 is other than lower alkoxy have utility as antihypertensive agents. Processes for preparing the quinolones and pharmaceutical compositions containing them are disclosed.
