Application of N-acetyl phenylalanine derivatives to inhibition of urease activity

Abstract

The invention discloses application of N-acetyl phenylalanine derivatives to the inhibition of urease activity, wherein the N-acetyl phenylalanine derivatives are discovered on the basis of a medicinal virtual screening platform which combines the bioinformatics and a computer technology. The N-acetyl phenylalanine derivatives have favorable inhibition activity to urease and have the advantages of simple structure, small toxic and side effects, easy synthesis, and the like, thereby having favorable development potential.

Description

technical field [0001] The present invention relates to the application of a class of small molecular organic compounds represented by the structure containing N-acetylated phenylalanine discovered through virtual screening based on bioinformatics and computing technology in inhibiting urease activity, and specifically relates to small molecular Use of compound N-acetylated phenylalanine derivatives for inhibiting urease activity. Background technique [0002] Urease widely exists in various bacteria, fungi, actinomycetes and plants, especially in soybeans and other legume feeds, where the activity is quite high. Urease helps plants and microorganisms use endogenous and exogenous urea as a nitrogen source, and can synthesize body protein from ammonia produced by decomposition. The presence of urease accelerates the decomposition of urea to release ammonia, which greatly reduces the utilization rate of nitrogen by animals and plants, causes the pH value of the soil to increa...

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Problems solved by technology

But so far, the mechanism of action of various urease inhibitors is not clear, and the effectiveness of many urease inhibitors is affected by factors such as temperature, time, and pH environment.

The main component of domestically mature urease inhibitor feed additive products is acetohydroxamic acid, which is a hydroxamic acid inhibitor discovered in 1962 that can inhibit urease activity. It is characterized by simple synthesis, low cost, and high toxicity. Low, with a certain effect, the main problem is that the rumen microorganisms can quickly adapt to this compound, after a week of feeding, the ammonia level in the rumen returned to the level at the beginning of the test, long-term use of acetohydroxamic acid, microorganisms produced Adaptability, acetohydroxamic acid loses its effect (Li Jie, Ge Wei, Research Progress of Ruminant Urease Inhibitors, Journal of Northeast Agricultural University, 2004, 35, 119-122)

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