Tag: M.W=350-400

Malakoutikhah, Morteza published the artcileN-Methyl Phenylalanine-Rich Peptides as Highly Versatile Blood-Brain Barrier Shuttles, HPLC of Formula: 158922-07-7, the main research area is blood brain barrier delivery peptide drug.

Here we studied the capacity of N-MePhe-(N-MePhe)3-CONH2, Cha-(N-MePhe)3-CONH2, and 2Nal-(N-MePhe)3-CONH2 to carry various drugs (cargos) in in vitro blood-brain barrier (BBB) models in order to determine the versatility of these peptides as BBB-shuttles for drug delivery to the brain. Using SPPS, the peptides were coupled to GABA, Nip, and ALA to examine their passive BBB permeation by means of PAMPA and their lipophilicity by IAMC. Unaided, these nonpermeating drugs alone did not cross the PAMPA barrier and the BBB passively; however, the peptides tested as potential BBB shuttles transferred them by passive transfer through the PAMPA phospholipid. The permeability of peptides that showed the highest permeability in PAMPA, and Ac-N-MePhe-(N-MePhe)3-CONH2 as the parent peptide was also examined in bovine brain microvessel endothelial cells (BBMECs). These peptide-based BBB shuttles open up the possibility to overcome the formidable obstacle of the BBB, thereby achieving drug delivery to the brain.

Journal of Medicinal Chemistry published new progress about Biological permeation. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, HPLC of Formula: 158922-07-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Hamper, Bruce C. published the artcileSolid Phase Synthesis of β-Peptoids: N-Substituted β-Aminopropionic Acid Oligomers, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, the main research area is solid phase preparation peptoid combinatorial library; substituted aminopropionic acid oligomer library preparation.

A solid-phase organic synthesis method has been developed for the preparation of N-substituted-β-aminopropionic acid oligomers or β-peptoids I. Treatment of polymer-bound 4-(benzyloxy)benzyl acrylate with primary amines afforded N-substituted β-alanines. Polymer loadings and product conversions were determined by direct cleavage of resin-bound materials and measurement by 1H NMR with an internal standard The NMR method was used to establish loading of all resin-bound intermediates including acrylic acid. Acylation with acryloyl chloride followed by Michael addition of primary amines to the acrylamide allowed preparation of di-β-peptoids. By a linear set of seven reactions, trimeric N-benzyl-β-aminopropionic acid was prepared in 67% overall yield. Single-bead FT-IR microspectroscopy was used to acquire spectra of the resin bound mono-β-peptoids, di-β-peptoids, and acrylamide intermediates. A combinatorial library of defined mixtures of tri-β-peptoids was prepared by mixing equimolar amounts of the mono-β-peptoid resins and carrying them through two sequences of the acylation-Michael addition The identity of a sample mixture II (R = Me, CH2Ph, CH2CH2Ph, CH2C6H4OMe-4, allyl, CH2CHMe2, CHMeEt, CHMe2) was determined by LC-MS anal. of the cleavage product.

Journal of Organic Chemistry published new progress about Combinatorial chemistry. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Dolle, Roland E. published the artcileA statistical-based approach to assessing the fidelity of combinatorial libraries encoded with electrophoric molecular tags. Development and application of tag decode-assisted single bead LC/MS analysis, COA of Formula: C21H21NO4, the main research area is statistical sampling mol tag encoded combinatorial library statine amide; combinatorial library QA method tag decoding single bead LCMS; statine peptide library preparation inhibition screening cathepsin plasmepsin.

A statistical sampling protocol is described to assess the fidelity of libraries encoded with mol. tags. The methodol., termed library QA, is based on the combined application of tag decode anal. and single bead LC/MS. The phys. existence of library compounds eluted from beads is established by comparing the mol. weight predicted by tag decode with empirical measurement. The goal of sampling is to provide information on overall library fidelity and an indication of the performance of individual library synthons. The minimal sampling size n for library QA is 10× the largest synthon set. Data are reported as proportion (p) ± lower and upper boundary (lb-ub) computed at the 95% confidence level (α = 0.05). As a practical demonstration, library QA was performed on a 25 200-member library of statine-containing peptide amides (size = 40 × 63 × 10). Sampling was conducted three times at n ∼ 630 beads per run for a total of 1902 beads. The overall proportions found for the three runs were consistent with one another: p = 84.4%, lb-ub = 81.5-87.2%; p = 83.1%, lb-ub = 80.2-85.95; and p = 84.5%, lb-ub = 81.8-87.3%, suggesting the true value of p is close to 84% compound confirmation. The performance pi of individual synthons was also computed. Corroboration of QA data with biol. screening results obtained from assaying the library against cathepsin D and plasmepsin II is discussed.

Journal of Combinatorial Chemistry published new progress about Combinatorial chemistry. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, COA of Formula: C21H21NO4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Vojkovsky, Tomas published the artcileDetection of secondary amines on solid phase, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, the main research area is Merrifield synthesis chloranil monitoring; amine secondary detection Merrifield synthesis.

The detection of secondary amino groups in building blocks attached to solid phase using tetrachlorobenzoquinone (chloranil) was re-examined A new procedure, about ten times more sensitive than the original method, has been developed. Except for N-p-tolylglycine, all secondary amino groups that were examined were detected reliably in a substitution range down to 2.8 μeq/g. Protected imidazole in His(Trt) did not interfere with the detection method.

Peptide Research published new progress about Solid phase synthesis, solid-phase peptide synthesis. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zheng, Changsheng published the artcileA General Method for the Solid-Phase Synthesis of Unsymmetrical Tri- and Tetrasubstituted Ureas, Product Details of C21H21NO4, the main research area is urea unsym solid phase preparation.

A general method for the preparation of unsym. di-, tri-, and tetrasubstituted ureas on polymer supports is presented. Polymer-bound primary and secondary amines react with imidazolium salts (urea donors), which are generated from the reaction of N,N’-carbonyldiimidazole with primary and secondary amines followed by alkylation with MeI to give tri- and tetrasubstituted ureas in excellent yields (76-98%) and purities (80-99%).

Journal of Combinatorial Chemistry published new progress about Primary amines Role: RCT (Reactant), RACT (Reactant or Reagent). 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Product Details of C21H21NO4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Song, Aimin published the artcileA Novel and Rapid Encoding Method Based on Mass Spectrometry for “”One-Bead-One-Compound”” Small Molecule Combinatorial Libraries, SDS of cas: 158922-07-7, the main research area is combinatorial library decoding technique mass spectrometry; solid phase synthesis decoding combinatorial library mass spectroscopy; coding block synthesis deconvolution combinatorial library solid phase; single bead decoding combinatorial library.

A method for the preparation and encoding of readily deconvoluted combinatorial libraries is discussed. Beads are prepared with topol. segregated regions – an inner region to which is bound coding tags and an outer segment to which the library compound is bound. Coding blocks are attached to the inner resin by a cleavable methionine-containing linker; the coding blocks are chosen to have similar reactivities to the building blocks incorporated in the synthesis of the combinatorial library. Synthesis of the library leads to the functionalization of the library-containing portion of the resin bead and the coding portion of the resin bead. Cleavage of the linkers for the coding blocks from the resin bead by Edman degradation with cyanogen bromide yields lactones whose mass is determined by FT-MALDI mass spectroscopy. Anal. of the lactones isolated from a given bead yields the mass of each of the fragments present; by careful choice of coding blocks and reactants, the identities of the building blocks incorporated into a library bead and of the library member attached to that bead can be readily derived from the fragment masses. A combinatorial library is prepared and tested for the binding of library members to streptavidin; seventeen of the compounds are found to bind strongly to streptavidin by a colorometric assay and identified unambiguously by the library encoding method described here.

Journal of the American Chemical Society published new progress about Amines Role: CMB (Combinatorial Study), RCT (Reactant), RACT (Reactant or Reagent). 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, SDS of cas: 158922-07-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Barry, Grant D. published the artcileNovel Agonists and Antagonists for Human Protease Activated Receptor 2, Category: piperidines, the main research area is dipeptide isoxazolylcarbonyl preparation human PAR2 agonist antagonist SAR; human protease activated receptor 2 agonist antagonist dipeptide preparation.

Human protease activated receptor 2 (PAR2) is a G protein-coupled receptor that is associated with inflammatory diseases and cancers. PAR2 is activated by serine proteases that cleave its N-terminus and by synthetic peptides corresponding to the new N-terminus. Peptide agonists are widely used to characterize physiol. roles for PAR2 but typically have low potency (e.g., SLIGKV-NH2, SLIGRL-NH2), uncertain target selectivity, and poor bioavailability, limiting their usefulness for specifically interrogating PAR2 in vivo. Structure-activity relationships were used to derive new PAR2 agonists and antagonists containing nonpeptidic moieties. Agonist I (EC50 0.28 μM) selectively induced PAR2-, but not PAR1-, mediated intracellular Ca2+ release in HT29 human colorectal carcinoma cells. Antagonist II (IC50 2 μM) is the first compound at micromolar concentrations to reversibly inhibit PAR2 activation by both proteases and other PAR2 agonists (e.g., trypsin, 2f-furoyl-LIGRLO-NH2, I). The new compounds were selective for PAR2 over PAR1, serum stable, and suitable for modulating PAR2 in disease models.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kulkarni, Santosh S. published the artcileDesign and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, the main research area is metabotropic glutamate receptor subtype 5 antagonist aroylaminopyridine aroylaminothiazole preparation.

A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.

Bioorganic & Medicinal Chemistry Letters published new progress about. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Recommanded Product: 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

El Oualid, Farid published the artcileA Combinatorial Approach toward the Generation of Ambiphilic Peptide-Based Inhibitors of Protein:Geranylgeranyl Transferase-1, Quality Control of 158922-07-7, the main research area is protein geranylgeranyl transferase inhibitor peptide combinatorial solid phase preparation.

A combinatorial synthesis of oligopeptide analogs and their evaluation as protein geranylgeranyl transferase inhibitors is presented. The combinatorial strategy is based on the random mutation, in each new generation, of one of any of the four amino acid building blocks of which the most effective compounds of the previous generation are assembled. In this way, a progressive improvement of the average inhibitory activity was observed until the fifth generation. The most active inhibitors were found to inhibit PGGT-1 in the low micromolar range (IC50 = 3.8-8.1 μM).

Journal of Combinatorial Chemistry published new progress about Combinatorial chemistry, solid-phase. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, Quality Control of 158922-07-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Coleman, David R. published the artcileInvestigation of the Binding Determinants of Phosphopeptides Targeted to the Src Homology 2 Domain of the Signal Transducer and Activator of Transcription 3. Development of a High-Affinity Peptide Inhibitor, COA of Formula: C21H21NO4, the main research area is phosphopeptide preparation structure activity inhibitor Stat3 SH2 domain.

As part of their research on the design of Src homol. 2 (SH2) directed peptidomimetic inhibitors of Stat3, the authors, here, describe structure-activity relationship studies that provide information on the nature of peptide-protein interactions of a high-affinity phosphopeptide, Ac-Tyr(PO3H2)-Leu-Pro-Gln-Thr-Val-NH2 (peptide 1), inhibitor of Stat3 dimerization and DNA binding. There is a hydrophobic surface on the SH2 domain that can accommodate lipophilic groups on the N-terminus. Of the amino acids tested, leucine provided the highest affinity at pY+1 and its main chain NH is involved with a hydrogen bond with Stat3, presumably Ser636. Cis-3,4-Methanoproline is optimal as a backbone constraint at pY+2. The side chain amide protons of Gln are required for high-affinity interactions. The C-terminal dipeptide, Thr-Val, can be replaced with groups ranging in size from Me to benzyl. The authors synthesized a phosphopeptide incorporating groups that provided increases in affinity at each position. Thus, Ph(CH2)2CO-Tyr(PO3H2)-Leu-cis-3,4-methanoPro-Gln-NHCH2Ph was the highest affinity peptide, exhibiting an IC50 of 125 nM vs. 290 nM for peptide 1 in a fluorescence polarization assay.

Journal of Medicinal Chemistry published new progress about Protein motifs, SH2 domain. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, COA of Formula: C21H21NO4.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem