Radical cyclizations of alkenyl acylphosphonate derivatives under thermal and photochemical conditions
The use of alkenyl acylphosphonate and acylphosphine oxide derivatives as acceptors in radical cyclizations was studied under thermal and photochemical conditions, respectively. The cyclizations of alkenyl acylphosphonates under thermal conditions occurre
Design and synthesis of conformationally constrained 3-(N-alkylamino) propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors
A series of conformationally constrained analogs of 3 were synthesized and evaluated as S1P receptor agonists. Several novel scaffolds were identified as suitable for further investigation. A series of conformationally constrained 3-(N-alkylamino)propylphosphonic acids were systematically synthesized and their activities as S1P receptor agonists were evaluated. Several pyrrolidine and cyclohexane analogs had S1P receptor profiles comparable to the acyclic lead compound, 3-(N-tetradecylamino)propylphosphonic acid (3), lowered circulating lymphocytes in mice after iv administration and were thus identified as being suitable for further investigations.
Yan, Lin,Hale, Jeffrey J.,Lynch, Christopher L.,Budhu, Richard,Gentry, Amy,Mills, Sander G.,Hajdu, Richard,Keohane, Carol Ann,Rosenbach, Mark J.,Milligan, James A.,Shei, Gan-Ju,Chrebet, Gary,Bergstrom, James,Card, Deborah,Rosen, Hugh,Mandala, Suzanne M.
p. 4861 - 4866
(2007/10/03)
EPSP SYNTHASE: THE DESIGN AND SYNTHESIS OF BISUBSTRATE INHIBITORS INCORPORATING NOVEL 3-PHOSPHATE MIMICS
Novel aromatic bisubstrate inhibitors of the enzyme EPSP (5-enolpyruvoylshikimate-3-phosphate) synthase (EC 2.5.1.19) have been designed and synthesized as structural analogs of the single, catalytic intermediate 1 utilized by the enzyme.These aromatic inhibitors incorporate novel α-hydroxyphosphonates, malonate ethers and α-hydroxymalonates as replacements for the hydrolytically labile 3-phosphate group.These 3-phosphate mimics were much preferred to the corresponding methylene and vinylic phosphonates, malonates and phosphonomethyl ethers.
Sikorski, James A.,Miller, Michael J.,Braccolino, Diane S.,Cleary, Darryl G.,Corey, Susan D.,et al.
p. 115 - 118
(2007/10/02)
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