Application of bisindolyl pyrrole compound
A compound, selected technology, applied in application, animal repellent, plant growth regulator, etc., can solve problems such as limiting the growth and development of fungal arthropods
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Embodiment 1
[0057]Example 1 Determination of the inhibitory rate of bisindole pyrrole compounds to chitinase OfHex1, OfChi-h, OfChtI and OfChtII
[0058] The inhibitory activity of the compounds against chitinases OfHex1, OfChi-h, OfChtI and OfChtII was determined.
[0059] Positive control: Set up 3 parallel positive controls. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L chitinase and 50μM MU-GlcNAc or 20μM MU-(GlcNAc) 2 Incubate in 20mmol / L pH 6.0 phosphate buffer for 30min, then add 100μL 0.5mol / L sodium carbonate solution to terminate the reaction, and measure the absorbance value at 450nm wavelength after the reaction solution is excited with excitation light of 360nm wavelength.
[0060] Experimental group: set up 3 parallel experimental groups. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L chitinase, 10μM compound and 50μM MU-GlcNAc or 20μM MU-(GlcNAc) 2 Incubate in 20mmol / L pH 6.0 phosphate buffer for 30...
Embodiment 2
[0067] Example 2 Determination of Inhibition Constants of Bisindole Pyrrole Compounds to Chitinase
[0068] Three sets of substrate concentration gradients were set up for the reaction, MU-(GlcNAc) 2 As substrates, three sets of substrate concentration gradients were set up for the reaction, and the final concentrations were 5 μM, 10 μM and 20 μM, respectively. Under each group of substrate concentrations, multiple groups of suitable compound concentration gradients were taken to measure the inhibitory activity. The reaction system is 100 μL, the buffer environment is 20 mM phosphate buffer, pH 6.0, the final enzyme concentration is 2 nM, the reaction temperature is 30 ° C, the reaction time is 30 min, and then 100 μL of 0.5 M sodium carbonate solution is added to terminate the reaction, and the released MU passes through The absorbance value was measured at a wavelength of 450nm after excitation with 360nm excitation light. The data is plotted by Dixon method, the K of comp...
Embodiment 3
[0069] Embodiment 3 insecticidal activity
[0070] Select the armyworm on the first day of the third instar to carry out the experiment, mix the compound 10 dissolved in ethanol into the feed, and feed (inhibitor concentration in the feed: 0mM, 2.5mM, 10mM, 1g feed=1ml water), each group feeds 30 worms continued to observe the living conditions of armyworms during feeding and recorded them. Such as figure 2 Figures A, B, and C show the death curves and phenotypes of armyworms fed with different concentrations of compound 10. When the compound 10 was fed at a concentration of 10 mM, armyworms died in large numbers on the third day, and all died on the fourth day. When dead, the worms are small and shriveled. When compound 10 was fed at a concentration of 2.5 mM, the growth rate of armyworms slowed down significantly, and the mortality rate became higher and higher with time. Growth returned to normal when normal feed was subsequently fed. Such as figure 2 As shown in D,...
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