212838-70-5Relevant articles and documents
Isotopically Directed Symmetry Breaking and Enantioenrichment in Attrition-Enhanced Deracemization
Blackmond, Donna G.,Houk, K. N.,Murray, James I.,Richardson, Paul F.,Sanders, Jacob N.
supporting information, (2020/03/10)
The evolution of homochirality via attrition-enhanced deracemization (AED) of enantiomorphic solids is carried out using molecules that differ only in the isotopic composition of a phenyl group positioned remote from the chiral center. Enantioenrichment c
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach
Zhan, Peng,Chen, Wenmin,Li, Zhenyu,Li, Xiao,Chen, Xuwang,Tian, Ye,Pannecouque, Christophe,Clercq, Erik De,Liu, Xinyong
, p. 6795 - 6802 (2013/01/15)
The present work is an extension of our ongoing efforts towards the development and identification of new molecules with anti-HIV activity which have previously led to the discovery of arylazolylthioacetanilides as highly active NNRTIs. In this article, a series of 2-2-(3-(2-chlorophenyl)pyrazin-2- ylthio)-N-arylacetamide derivatives were synthesized and evaluated for in vitro anti-HIV activity. Most of the tested compounds exhibited moderate activities against wild-type HIV-1. Among them, compound 6k showed significant activity against wild-type HIV-1 with an EC50 value of 1.7 μM, along with moderate activity against wild-type reverse transcriptase (RT). The preliminary structure-activity relationship (SAR) and docking calculations of this new series of compounds were also investigated, which may help designing more potent molecules.