391680-79-8Relevant articles and documents
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.
Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid
Stansfield, Ian,Avolio, Salvatore,Colarusso, Stefania,Gennari, Nadia,Narjes, Frank,Pacini, Barbara,Ponzi, Simona,Harper, Steven
, p. 5085 - 5088 (2007/10/03)
The discovery of a simple 2-thienyl substituted 5,6-dihydroxypyrimidine-4- carboxylic acid active-site inhibitor of the HCV NS5B polymerase inhibitor is reported. Structure-activity relationships that led to an understanding of the pharmacophore around the pyrimidine ring is also described.
