60458-71-1Relevant academic research and scientific papers
Discovery and optimization of selective inhibitors of meprin α (Part ii)
Wang, Chao,Diez, Juan,Park, Hajeung,Spicer, Timothy P.,Scampavia, Louis D.,Becker-Pauly, Christoph,Fields, Gregg B.,Minond, Dmitriy,Bannister, Thomas D.
, p. 1 - 17 (2021)
Meprin α is a zinc metalloproteinase (metzincin) that has been implicated in multiple dis-eases, including fibrosis and cancers. It has proven difficult to find small molecules that are capable of selectively inhibiting meprin α, or its close relative meprin β, over numerous other metzincins which, if inhibited, would elicit unwanted effects. We recently identified possible molecular starting points for meprin α-specific inhibition through an HTS effort (see part I, preceding paper). Here, in part II, we report further efforts to optimize potency and selectivity. We hope that a hydroxamic acid meprin α inhibitor probe will help define the therapeutic potential for small molecule meprin α inhibition and spur further drug discovery efforts in the area of zinc metalloproteinase inhibition.
Microwave-assisted synthesis and antifungal activity of novel 1,2,4-triazole thioether derivatives containing pyrimidine moiety
Xu, Meng,Zhu, Ya-Bo,Wang, Mei,Khan, Ikhlas A.,Liu, Xing-Hai,Weng, Jian-Quan
, p. 347 - 352 (2018/04/20)
Background: Plant diseases caused by plant pathogens are important constraints to agricultural production throughout the world and at least 10% of global food production is lost to plant diseases. In order to discover new fungicides and control the plant
2-substituted benzylthio-5-(4,6-dimethyl pyrimidine-2-)thiomethyl-1,3,4-oxadiazole compound and application thereof
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, (2016/10/10)
The invention relates to a 2-substituted benzylthio-5-(4,6-dimethyl pyrimidine-2-)thiomethyl-1,3,4-oxadiazole compound and an application thereof. The compound provided by the invention is easy to prepare, and the aftertreatment is convenient; and the obtained compound is used as a bactericide against gotryis cinerea, fusarium oxysporum, fungus colletorichum acutatum, strawberry anthracnose or colletotrichum gloeosporioides and shows relatively good bacteriostatic activity.
4-phenyl-3-((4,6-dimethylpyrimidin-2-yl thio)methyl)-5-benzylthio triazole compounds and application thereof
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, (2016/10/17)
The invention relates to 4-phenyl-3-((4,6-dimethylpyrimidin-2-yl thio)methyl)-5-benzylthio triazole compounds and an application thereof; in the compounds, compounds having nonsubstituted H in a benzene ring show a certain inhibitory activity on all tested strains; the compounds Ia (Rn=p-cyano), Ib (Rn=p-bromo) and Ic (Rn=p-chloro) have all the inhibition rates on colletrichum orbiculare of more than or equal to 50%, wherein the inhibition rate of Ic is 73.24%; the compounds Ia (Rn=p-cyano), Ib (Rn=p-bromo), Ic (Rn=p-chloro) and Ih (Rn=o-chloro) have all the inhibition rates on botrytis cinerea of more than or equal to 40%; the compounds Ia (Rn=p-cyano), Ib (Rn=p-bromo) and Ic (Rn=p-chloro) have all the inhibition rates on rhizoctonia solani of more than or equal to 50%, wherein the inhibition rate of Ic is 66.37%.
2-substituted benzylthio-5-(4,6-dimethyl pyrimidine-2-)sulfur methyl-1,3,4-thiadiazole compound and application thereof
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, (2016/10/17)
The invention relates to a 2-substituted benzylthio-5-(4,6-dimethyl pyrimidine-2-)sulfur methyl-1,3,4-thiadiazole compound and application thereof. The compound is simple in preparation method, after-treatment is convenient, and the obtained compound has obvious effects when applied as bactericide for botryis cinerea, fusarium oxysporum, fungus colletorichum acutatum, strawberry anthracnose and colletotrichum gloeosporioides.
Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction
Reddy, Tummala R.K.,Li, Chan,Guo, Xiaoxia,Fischer, Peter M.,Dekker, Lodewijk V.
, p. 5378 - 5391 (2014/12/11)
Recent target validation studies have shown that inhibition of the protein interaction between annexin A2 and the S100A10 protein may have potential therapeutic benefits in cancer. Virtual screening identified certain 3,4,5-trisubstituted 4H-1,2,4-triazoles as moderately potent inhibitors of this interaction. A series of analogues were synthesized based on the 1,2,4-triazole scaffold and were evaluated for inhibition of the annexin A2-S100A10 protein interaction in competitive binding assays. 2-[(5-{[(4,6-Dimethylpyrimidin-2-yl)sulfanyl]methyl}-4-(furan-2-ylmethyl)-4H-1,2,4-triazol-3-yl)sulfanyl]-N-[4-(propan-2-yl)phenyl]acetamide (36) showed improved potency and was shown to disrupt the native complex between annexin A2 and S100A10.
