Modular construction of quaternary hemiaminal-based inhibitor candidates and their in cellulo assessment with HIV-1 protease

…, P Maurin, R Wolkowicz, P Falson, J Hasserodt

Index: Gros, Guillaume; Martinez, Lorena; Gimenez, Anna Servat; Adler, Paula; Maurin, Philippe; Wolkowicz, Roland; Falson, Pierre; Hasserodt, Jens Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 17 p. 5407 - 5413

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Citation Number: 3

Abstract

Abstract Non-peptidomimetic drug-like protease inhibitors have potential for circumventing drug resistance. We developed a much-improved synthetic route to our previously reported inhibitor candidate displaying an unusual quaternized hemi-aminal. This functional group forms from a linear precursor upon passage into physiological media. Seven variants were prepared and tested in cellulo with our HIV-1 fusion-protein technology that result in an ...