Zhu, Mei published the artcileNovel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants, Application of 2-Morpholinoethanol, the publication is ACS Medicinal Chemistry Letters (2020), 11(6), 1196-1204, database is CAplus and MEDLINE.
Flexible heterocyclic moieties as the P2 ligands of HIV-1 protease inhibitors may be adapted to the minimally distorted active site of mutations easily and enhance activity against DRV-resistant HIV-1 variants. Herein, the design, synthesis, and biol. evaluation of a new series of inhibitors containing morpholine derivatives as the P2 ligands were described, among which, carbamate inhibitor I and carbamido inhibitor II exhibited almost 4- and 2-fold superior activity with enzyme Ki of 0.092 nM and 0.21 nM, as well as antiviral IC50 values of 0.41 nM and 0.95 nM, resp., compared to DRV. Besides, they exhibited excellent activity with inhibition of 94% and 91%, resp. Furthermore, they also showed appreciable antiviral activity against DRV-resistant HIV-1 variants.
ACS Medicinal Chemistry Letters published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C8H6BrF3S, Application of 2-Morpholinoethanol.
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