Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, new energy materials, nano-ceramics, nano-hybrid composite materials, preparation and modification of special coatings, In an article, 126456-43-7, name is (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol, introducing its new discovery. Recommanded Product: 126456-43-7
Structure-Based Design of Novel HIV Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors
The low oral bioavailability and rapid biliary excretion of peptide-derived HIV protease inhibitors have limited their utility as potential therapeutic agents.Our broad screening program to discover nonpeptidic HIV protease inhibitors had previously identified compound II (phenprocoumon, Ki = 1 muM) as a lead template.Crystal structures of HIV protease complexes containing the peptide-derived inhibitor I (1-(naphthoxyacetyl)-L-histidyl-5(S)-amino-6-cyclohexyl-3(R),4(R)-dihydroxy-2(R)-isopropylhexanoyl-L-isoleucine N-(2-pyridylmethyl)amide) and nonpeptidic inhibitors, such as phenprocoumon (compound II), provided a rational basis for the structure-based design of more active analogues.This investigation reports on the important finding of a carboxamide functionality appropriately added to the 4-hydroxycoumarin and the 4-hydroxy-2-pyrone templates which resulted in new promising series of nonpeptidic HIV protease inhibitors with improved enzyme-binding affinity.The most active diastereomer of the carboxamide-containing compound XXIV inhibited HIV-1 protease with a Ki value of 0.0014 muM.This research provides a new design direction for the discovery of more potent HIV protease inhibitors as potential therapeutic agents for the treatment of HIV infection.
Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amountRecommanded Product: 126456-43-7, you can also check out more blogs about126456-43-7
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Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis