62222-38-2Relevant academic research and scientific papers
Pharmacophore requirements for HIV-1 reverse transcriptase inhibitors that selectively “Freeze” the pre-translocated complex during the polymerization catalytic cycle
Lacbay, Cyrus M.,Menni, Michael,Bernatchez, Jean A.,G?tte, Matthias,Tsantrizos, Youla S.
, p. 1713 - 1726 (2018/02/27)
Reverse transcriptase (RT) is responsible for replicating the HIV-1 genome and is a validated therapeutic target for the treatment of HIV infections. During each cycle of the RT-catalyzed DNA polymerization process, inorganic pyrophosphate is released as the by-product of nucleotide incorporation. Small molecules were identified that act as bioisosteres of pyrophosphate and can selectively freeze the catalytic cycle of HIV-1 RT at the pre-translocated stage of the DNA- or RNA-template-primer-enzyme complex.
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: Design, biochemical activity, and structural information
Kirschberg, Thorsten A.,Balakrishnan, Mini,Squires, Neil H.,Barnes, Tiffany,Brendza, Katherine M.,Chen, Xiaowu,Eisenberg, Eugene J.,Jin, Weili,Kutty, Nilima,Leavitt, Stephanie,Liclican, Albert,Liu, Qi,Liu, Xiaohong,Mak, John,Perry, Jason K.,Wang, Michael,Watkins, William J.,Lansdon, Eric B.
supporting information; experimental part, p. 5781 - 5784 (2010/03/24)
Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These molecules can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymatic activity was measured in a biochemical assay, but no antivira
HCV NS5b RNA-dependent RNA polymerase inhibitors: From α,γ- diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5- hydroxypyrimidinonecarboxylic acids. Design and synthesis
Summa, Vincenzo,Petrocchi, Alessia,Matassa, Victor G.,Taliani, Marina,Laufer, Ralph,De Francesco, Raffaele,Altamura, Sergio,Pace, Paola
, p. 5336 - 5339 (2007/10/03)
A new class of the HCV NS5b RNA-dependent RNA polymerase inhibitors, the dihyroxypyrimidinecarboxylic acid derivative, was designed from a diketoacid and meconic acid derivative discovered by screening. Mechanism of action and essential moieties required for activity were identified. The corresponding N-methylpyrimidinone was also prepared; both classes are novel, reversible, and selective inhibitors of the HCV NS5b polymerase with improved druglike characteristics.
Highly selective synthesis of 2-substituted-5-hydroxy-6-oxo-1,6- dihydropyrimidine-4-carboxylic acid derivatives using a novel protected dihydroxyfumarate
Dreher, Spencer D.,Ikemoto, Norihiro,Gresham, Venita,Liu, Jinchu,Dormer, Peter G.,Balsells, Jaume,Mathre, David,Novak, Thomas J.,Armstrong III, Joseph D.
, p. 6023 - 6025 (2007/10/03)
A high yielding (50-96%) route to 2-substituted-5-hydroxy-6-oxo-1,6- dihydropyrimidine-4-carboxylic acid derivatives has been developed using a rationally designed dihydroxyfumarate derivative. The fully unprotected pyrimidinone heterocycle was prepared i
