Category: 158922-07-7

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

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

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

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