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Showing 1 to 18 of 18 for “"isosteres"”.
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Synthesis of D-alanyl-D-alanine dipeptide isosteres and cephalosporin prodrugs
… peptidoglycan cell wall. Synthesis of dipeptide isosteres which may be incorporated into the growing cell wall is described. Previously published syntheses were employed as well as a Wittig reaction using a chiral Wittig reagent, a reaction not used in the synthesis of isosteres before. If the …
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I Progress towards the synthesis of plakortether B through a zinc-mediated homologation II Synthesis of novel hydroxy-cyclopropyl peptides isosteres
… bicyclic lactones as precursors to peptide isosteres.</p>
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Triazole-linked reduced amide isosteres: An approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors and NH-assisted Fürst-Plattner opening of cyclohexene oxides
… to discover 4 triazole-linked reduced amide isosteres that showed modest (single digit micromolar) BACE1 inhibition. Our ligands were designed based on a very potent (single digit nanomolar) isopththalamide ligand from Merck. We supplanted one of the amide linkages in order to incorporate our …
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I.~Design, Synthesis, and Evaluation of a Rigidly Constrained Peptidomimetic as a Potential Type I Beta-Turn. II.~Development of Novel Estrogen Receptor Ligands With Unique Endocrine Profiles. III.~Design, Synthesis and Biological Evaluation of Potential Aspartic Protease Inhibitors Based on the Diaziridine and Diazirine Isostere
… enzyme mediated peptide bond hydrolysis. These isosteres (143 and 144) have been incorporated into substrates for the aspartic protease pepsin, however they did not show any inhibition.
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Design, Syntheses, and Bioactivities of Conformationally Locked Pin1 Ground State Inhibitors
… of Pin1 using molecular probes, two amide isosteres of Ser-<i>trans</i>-Pro and Ser-<i>cis</i>-Pro dipeptides were designed and stereoselectively synthesized. The conformationally locked Ser–<i>trans</i>–Pro mimic, Boc-SerΨ[(<i>E</i>)CH=C]Pro–OH, was synthesized through the use of an …
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Antiviral Agents: 3,5-Disubstituted 1,2,4-Oxadiazole Derivatives and Novel Peptidomimetics Containing Hydroxyethyl Isostere and Imidazolidinone Structures
… from both imidazolidinones and hydroxyethylene isosteres is described herein. The key step of their synthesis is the opening of a fused ring aziridine with amino acids or small peptides to form an oxazolidinone, followed by rearrangement to the target imidazolidinone. A chain elongation on the …
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Études numérique et expérimentale des cycles à adsorption fonctionnant avec des nouveaux réfrigérants HCFC
… du couple charbon actif-methanol. Les isosteres des couples zeolite-R124, charbon actif-R123 et charbon actif-R124/R123 sont ensuite etablies experimentalement et ce modele numerique est utilise pour predire le comportement des cycles avec ces couples. L'etude de la comparaison des …
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Trifluoromethyl ketones: Potential insecticides towards Anopheles gambiae
… directed at synthesis of oxime and hydrazone TFK isosteres to determine the mechanism of action of these compounds.
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Convergent Site-Selective Carbohydrate-Peptide Ligations With Dehydroalanine and Aziridine -2 -Carboxylic Acid-Containing Peptides
… was demonstrated by the preparation of thio-isosteres of the four tumor-associated carbohydrate antigens, T N, T, STN, and 2,6-ST, as a pair of diastereoisomers at the newly formed cysteine stereocenter. This 1,4-conjugate addition ligation proceeded in high yield and with retention of …
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Isomerization-Locked Alkene Analogues of Xaa–Pro Dipeptides in the Proteins Collagen and Bora
… namely the n→π* interaction. Halo-alkene isosteres may be used to recapture these electronic interactions and stabilize a collagen-like peptide. An in-depth conformational analysis was conducted at the MP2/6-311+G(2d,p) level of theory to determine the viability of conformationally-locked …
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New methods for the asymmetric synthesis of α-alkylated ketones and 1,3-amino alcohols
… 2-heptyl-4-hydroxy-quinoline (HHQ) and possible isosteres of PQS; the C-3 Cl, Br and I analogues. N-Methylation of the iodide was also feasible and the usefulness of this compound showcased in Pd-catalysed cross-coupling reactions, thus allowing access to a diverse set of biologically important …
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Part 1 Design, Synthesis and Bioactivity of a Phosphorylated Prodrug for the Inhibition of Pin1; Part 2 Conformational Specificity of Cdc25c Substrate for Cdc2 Kinase using LC-MS/MS
… for the regulation of mitosis, two amide isosteres, Ser-Ψ[(Z)CH=C]-Pro-OH and Ser-Ψ[(E)CH=C]-Pro-OH were incorporated into two peptidomimetics derived from human Cdc25c. Phosphorylation of these two peptidomimetics by the incubation with Cdc2 was studied using LC-MS/MS technique. It was …
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Chlorinated amino acids in peptide production
… are primarily recognised by size exclusion, all isosteres with a methyl group replaced by similarly-sized chlorine are mistaken as substrates, and the ability of halogens to mimic the bonding interactions of sulfur enabled the design of a chlorinated and a brominated analogue of methionine. Amino …
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Chlorinated amino acids in peptide production
… are primarily recognised by size exclusion, all isosteres with a methyl group replaced by similarly-sized chlorine are mistaken as substrates, and the ability of halogens to mimic the bonding interactions of sulfur enabled the design of a chlorinated and a brominated analogue of methionine. Amino …
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Pin1 Inhibitors: Towards Understanding the Enzymatic Mechanism
… classes of designed inhibitors such as alkene isosteres, non-peptidic, small molecular Pin1 inhibitors, and indanyl ketones, and 2) several natural products such as juglone, pepticinnamin E analogues, PiB and its derivatives obtained from a library screen. These Pin1 inhibitors show promise in …
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I. Collagen-like polypeptides. II. Helix-turn-helix peptides and turn mimetics
… folding. The conformationally locked alkene isosteres Fmoc-Gly-Ψ[(E)CH=C]-Pro-Hyp(tBu)-OH and Fmoc-Pro-Ψ[(E)CH=C]-Pro-OH were designed and synthesized. The synthesis of the Gly-Pro isostere had no stereo-control, and the two diastereomers of the tripeptide isostere …
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Development of biotin protein ligase inhibitors from Staphylococcus aureus as new antibiotics
… using 1,2,3-triazole and acylsulfonamide isosteres to replace the phosphoroanhydride linker found in biotinyl-5’-AMP 1.03. Chapter one describes the structure and catalytic mechanism of the target enzyme SaBPL, along with an overview of chemical analogues of biotin and biotinyl-5’-AMP 1.03 …
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Design and synthesis of novel non peptidomimtic beta-secretase inhibitors in the treatment of Alzheimer's disease
… to explore the pseudopeptidic transition-state isosteres chemistry was carried out during research stage at Università de Montrèal (Canada) in Hanessian's group. The aim of this work has been the synthesis of the δ-aminocyclohexane carboxylic acid motif with stereochemically defined …