41128-92-1Relevant articles and documents
Synthesis, structure, and transformations of cyclic glycerol formals
Raskildina,Valiev,Sultanova,Zlotsky
, p. 2095 - 2099 (2015)
Glycerol reacts with paraformaldehyde to give a mixture of 4-hydroxymethyl-1,3-dioxolane and 5-hydroxy-1,3-dioxane. Some transformations (alkylation and replacement of the OH groups with the Cl atoms) of the synthesized compounds were performed. The differences in NMR and mass spectra of the corresponding 1,3-dioxolanes and 1,3-dioxanes were revealed and discussed.
Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: Design, synthesis, biological evaluation, and protein-ligand X-ray studies
Ghosh, Aran K.,Gemma, Sandra,Baldridge, Abigail,Wang, Yuan-Fang,Kovalevsky, Andrey Yu.,Koh, Yashiro,Weber, Irene T.,Mitsuya, Hiroaki
experimental part, p. 6021 - 6033 (2009/10/23)
We report the design, synthesis, and biological evaluation of a series of novel HIV-1 protease inhibitors. The inhibitors incorporate stereochemically defined flexible cyclic ethers/polyethers as high affinity P2-ligands. Inhibitors containing small ring 1,3-dioxacycloalkanes have shown potent enzyme inhibitory and antiviral activity. Inhibitors 3d and 3h are the most active inhibitors. Inhibitor 3d maintains excellent potency against a variety of multi-PI-resistant clinical strains. Our structure-activity studies indicate that the ring size, stereochemistry, and position of oxygens are important for the observed activity. Optically active synthesis of 1,3-dioxepan-5-ol along with the syntheses of various cyclic ether and polyether ligands have been described. A protein-ligand X-ray crystal structure of 3d-bound HIV-1 protease was determined. The structure revealed that the P2-ligand makes extensive interactions including hydrogen bonding with the protease backbone in the S2-site. In addition, the P2-ligand in 3d forms a unique water-mediated interaction with the NH of Gly-48.
PRODUCTS OF GLYCEROL CONDENSATION WITH ALDEHYDES
Teregulova, G. T.,Rol'nik, L. Z.,Zlot-skii, S. S.,Rakhmankulov, D. L.
, p. 1448 - 1451 (2007/10/02)
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