1007571-61-0Relevant articles and documents
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase
Chong, Pek,Sebahar, Paul,Youngman, Michael,Garrido, Dulce,Zhang, Huichang,Stewart, Eugene L.,Nolte, Robert T.,Wang, Liping,Ferris, Robert G.,Edelstein, Mark,Weaver, Kurt,Mathis, Amanda,Peat, Andrew
supporting information, p. 10601 - 10609 (2013/02/23)
A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole-amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallography of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led directly to the design of compound 43 that exhibits remarkable antiviral activity (EC50 1 nM) against a wide range of NNRTI-resistant viruses and a favorable pharmacokinetic profile across multiple species.
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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, (2009/01/20)
Compounds of formula (I), wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula (I) useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 33, (2008/06/13)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.