1189790-57-5Relevant articles and documents
Design, synthesis, and antiviral evaluation of chimeric inhibitors of HIV reverse transcriptase
Iyidogan, Pinar,Sullivan, Todd J.,Chordia, Mahendra D.,Frey, Kathleen M.,Anderson, Karen S.
, p. 1183 - 1188 (2013)
In a continuing study of potent bifunctional anti-HIV agents, we rationally designed a novel chimeric inhibitor utilizing thymidine (THY) and a TMC derivative (a diarylpyrimidine NNRTI) linked via a polymethylene linker (ALK). The nucleoside, 5′-hydrogen-phosphonate (H-phosphonate), and 5′-triphosphate forms of this chimeric inhibitor (THY-ALK-TMC) were synthesized and the antiviral activity profiles were evaluated at the enzyme and cellular level. The nucleoside triphosphate (11) and the H-phosphonate (10) derivatives inhibited RT polymerization with an IC50 value of 6.0 and 4.3 nM, respectively. Additionally, chimeric nucleoside (9) and H-phosphonate (10) derivatives reduced HIV replication in a cell-based assay with low nanomolar antiviral potencies.
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses
Cherukupalli, Srinivasulu,De Clercq, Erik,Fu, Zhipeng,Gao, Shenghua,Kang, Dongwei,Liu, Xinyong,Pannecouque, Christophe,Sun, Lin,Zhan, Peng,Zhang, Tao,Zhou, Zhongxia
, (2021)
To further explore the chemical space surrounding the “hydrophobic channel” of the NNRTI binding pocket (NNIBP), a new series of diarylpyrimidines (DAPYs) were designed and synthesized as potent HIV-1 non-nucleoside RT inhibitors (NNRTIs). The target comp
Substituted 1,2,3 triazole diarylpyrimidine derivative as well as preparation method and application thereof
-
, (2019/03/06)
The invention discloses a substituted 1,2,3 triazole diarylpyrimidine derivative as well as a preparation method and application thereof. The substituted 1,2,3 triazole diarylpyrimidine derivative orpharmaceutically acceptable salts or prodrugs thereof ha