1026977-99-0Relevant articles and documents
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1'phenyl substituents: X-ray crystal structure assisted design
Thompson,Fitzgerald,Holloway,Emini,Darke,McKeever,Schleif,Quintero,Zugay,Tucker,Schwering,Homnick,Nunberg,Springer,Huff
, p. 1685 - 1701 (1992)
By tethering of a polar hydrophilic group to the P1 or P1' substituent of a Phe-based hydroxyethylene isostere, the antiviral potency of a series of HIV protease inhibitors was improved. The optimum enhancement of anti-HIV activity was observed with the 4-morpholinylethoxy substituent. The substituent effect is consistent with a model derived from inhibitor docked in the crystal structure of the native enzyme. An X-ray crystal structure of the inhibited enzyme determined to 2.25 A verifies the modeling predictions.
α- and β-Substituted phosphonate analogs of LPA as autotaxin inhibitors
Cui, Peng,McCalmont, William F.,Tomsig, Jose L.,Lynch, Kevin R.,Macdonald, Timothy L.
, p. 2212 - 2225 (2008/09/21)
Autotaxin (ATX) is an attractive pharmacological target due to its lysophospholipase D activity which leads to the production of lysophosphatidic acid (LPA). Blockage of ATX produced LPA by small molecules could be a potential anticancer chemotherapy. In our previous study, we have identified the two β-hydroxy phosphonate analogs of LPA (compounds f17 and f18) as ATX inhibitors. With this work, we investigated α- and β-substituted phosphonate analogs of LPA and evaluated them for ATX inhibitory activity. The stereochemistry of β-hydroxy phosphonates was also studied.
Direct synthesis of N-protected β-amino dimethylhydroxamates: Application to the solid-phase synthesis of a peptide incorporating a new amide bond surrogate ψ[CH2CH2NH]
Limal, David,Quesnel, Anne,Briand, Jean-Paul
, p. 4239 - 4242 (2007/10/03)
A rapid and efficient one-step synthesis of N-protected β-amino dimethylhydroxamates starting from diazo ketones is reported. A Fmoc- protected β-amino aldehyde obtained by reduction of its corresponding dimethylhydroxamate was incorporated during solid p
SYNTHESIS OF FRAGMENTS OF THE VP1 PROTEIN OF TYPE A22 FOOT-AND-MOUTH DISEASE VIRUS. SYNTHESIS OF FRAGMENTS 134-139, 134-145, 140-145, 150-155, AND 150-159
Khalikov, Sh. Kh.,Alieva, S. V.,Ashurov, S. G.
, p. 202 - 212 (2007/10/02)
Fragments of peptides of the amino acid sequences (134-145) and (150-159) of the VP1 protein of the type A22 foot-and-mouth disease (FMD)virus have been synthesized by the classical methods of peptide chemistry.Oligopeptides were obt
