- N-phenylacetyl-L-proline preparation method
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The invention discloses an N-phenylacetyl-L-proline preparation method which includes the steps: dripping phenyl acetyl chloride and acid-binding agents into an organic solvent dissolved L-proline atlow temperature; adding a phase transfer catalyst, perfo
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Paragraph 0009; 0019; 0023; 0024; 0025; 0026
(2019/03/08)
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- Penicillin G acylase-mediated kinetic resolution of racemic 1-(N-acylamino)alkylphosphonic and 1-(N-acylamino)alkylphosphinic acids and their esters
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Extensive studies on the penicillin G acylase-mediated kinetic resolution of N-acylated 1-aminoalkylphosphonic and 1-aminoalkylphosphinic acids as well as their esters were carried out to recognise the relationships between the substrate structure, reacti
- Zielińska, Katarzyna,Mazurkiewicz, Roman,Szymańska, Katarzyna,Jarz?bski, Andrzej,Magiera, Sylwia,Erfurt, Karol
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- NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
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Page/Page column 236
(2011/07/06)
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- Synthesis and antiamnesic activity of a series of N-acylprolyl-containing dipeptides
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Eaters and amides of a series of N-acylprolyl-containing dipeptides were synthesized. It was established that these substances possess the ability to prevent memory decline evoked by maximal electroshock (MES) in a passive avoidance step-through paradigm. These N-acylprolyl-containing dipeptides were designed as analogues of pyroglutamyl-containing dipeptides, which we previously demonstrated to be highly active nootropics. Among the structure-activity relationships explored were the effect of N-acylsubstitution size, C-terminal substitution and the nature of the second amino acid. The optimal N-acyl moiety was the N-phenyl-acetyl group, while the optimal C-terminal substitution-esters were those derived from low alkyl alcohols. The optimal second amino acids were Asp, Glu or their fragments, Gly, β-Ala, GABA. Compound 1 (N-phenylacetylprolylglycine ethyl eater) was selected for further evalution in impaired cognitive functions. It was supposed that esters and unsubstituted amides of N-acylprolylglycines are prodrugs, which convert to the bioactive cyclo-(Pro-Gly) by virtue of enzymatic or chemical lability within the body.
- Gudasheva,Voronina,Ostrovskaya,Rozantsev,Vasilevich,Trofimov,Kravchenko,Skoldinov,Seredenin
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p. 151 - 157
(2007/10/03)
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- Design, synthesis, and testing of potential antisickling agents. 5. Disubstituted benzoic acids designed for the donor site and proline salicylates designed for the acceptor site
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This paper reports the discovery of a new class of potent antigelling agents. The new compounds, disubstituted benzoic acid derivatives, were designed by using molecular modeling experiments. These molecules contain functional groups positioned to interac
- Abraham,Gazze,Kennedy,Mokotoff
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p. 1549 - 1559
(2007/10/02)
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- Tri- and tetrapeptide analogues of kinins as potential renal vasodilators
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Tri- and tetrapeptide analogues were synthesized and evaluated as renal vasodilators. These peptides were prepared by standard coupling reactions which also provided good yields with hindered α-methyl amino acid derivatives. Preliminary evidence of renal vasodilator activity was determined in anesthetized dogs by measuring the effects on renal blood flow and calculating the accompanying changes in renal vascular resistance. The most potent compounds contained, in their structure, the L-prolyl-DL-α-methylphenylalanyl-L-arginine and L-prolyl-DL-α-methyl-phenyalanylglycyl-L-proline arrays. Substitution on the N-terminal proline with 4-phenylbutyryl and 4-(4-hydroxyphenyl)butyryl side chains produced enhanced renal vasodilator activity and, in certain cases, selectivity for the renal vasculature.
- Pfeiffer,Chambers,Hilbert,Woodward,Ackerman
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p. 325 - 341
(2007/10/02)
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- 1-Phenyl-2-aminoethanol derivatives
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The invention concerns compounds of the formula:- R1.CH(OH).CH2 NH.CR2 R3.A1. NH.CO.CHR4.A2.NR5. Q I wherein R1 is 3,4-bis[(3-8C)alkanoyloxy]-phenyl, 3,5- b
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