HIV-1 integrase inhibitor Chemical Properties

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

color 

Light yellow to yellow

HIV-1 integrase inhibitor Usage And Synthesis

Uses

HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

target

HIV-1 integrase

IC 50

HIV-1

References

[1] Hobaika, Z.; Zargarian, L.; Maroun, R. G.; Mauffret, O.; Burke, T. R., Jr.; Fermandjian, S. HIV-1 Integrase and Virus and Cell DNAs: Complex Formation and Perturbation by Inhibitors of Integration. Neurochemical Research (2010), 35(6), 888-893. DOI:10.1007/s11064-009-0098-2
[2] Loizidou, Eriketi Z.; Zeinalipour-Yazdi, Constantinos D.; Christofides, Tasos; Kostrikis, Leondios G. Analysis of binding parameters of HIV-1 integrase inhibitors: Correlates of drug inhibition and resistance. Bioorganic & Medicinal Chemistry (2009), 17(13), 4806-4818.
[3] Kawasuji T.Carbamoyl Pyridone HIV-1 Integrase Inhibitors. 1. Molecular Design and Establishment of an Advanced Two-Metal Binding Pharmacophore.J Med Chem. 2012 Sep 10. DOI:10.1021/jm3010459
[4] Yan A, Xuan S, Hu X.Classification of Active and Weakly Active ST Inhibitors of HIV-1 Integrase Using a Support Vector Machine.Comb Chem High Throughput Screen. 2012 Aug 28. DOI:10.2174/138620712803901108
[5] Yu S, Zhao G.Development of Polyphenols as HIV-1 Integrase Inhibitors: A Summary and Perspective.Curr Med Chem. 2012 Aug 27. DOI:10.2174/092986712803833236

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