85178-07-0

Upstream product

• 97-67-6 (S)-Malic acid 
• 100-51-6 benzyl alcohol 
• 617-48-1 malic acid 

Downstream Products

• 1369962-91-3 benzyl 2,4-dihydroxybutanoate 

Relevant academic research and scientific papers

PYRAZINE CARBAMATES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS

Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by GluN2B receptor activity.

PYRAZINE CARBAMATES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS

Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by GluN2B receptor activity.

OXADIAZOLE COMPOUNDS

Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.

5-methylmorpholine-3-amino-2-oxazolidone antigen and 5-methylmorpholine-3-amino-2-oxazolidone antibody, and preparation methods and applications thereof

The invention discloses a 5-methylmorpholine-3-amino-2-oxazolidone antigen and a 5-methylmorpholine-3-amino-2-oxazolidone antibody, and preparation methods and applications thereof. Reconstruction ofthe structure of a 5-methylmorpholine-3-amino-2-oxazolidone molecule, comprising introduction of a carbonyl structure, reduces the free rotation degree of the arm structure of a semi-antigen, so the semi-antigen has a conformation definiteness and an increased structure complexity, and the feature structure of the molecule is well recognized by an immunized animal, thereby the success probabilityof the preparation of the antibody is greatly increased. The 5-methylmorpholine-3-amino-2-oxazolidone artificial antigen and the 5-methylmorpholine-3-amino-2-oxazolidone artificial antibody are prepared on the basis of the semi-antigen, and the antigen and the antibody have a high tilter and a high detection efficiency, and solves the problems of long period, strong professional property, high cost, and unsuitableness for onsite large-batch rapid detection of traditional apparatus methods. The antigen and the antibody have the advantages of simple synthesis process, low cost, laying a foundation for the development of an enzyme-linked immune rapid detector having the characteristics of low cost, high detection efficiency and simplicity in operation, and good application prospect.

Design, Synthesis, and Characterization of Cyclic Peptidomimetics of the Inducible Nitric Oxide Synthase Binding Epitope That Disrupt the Protein-Protein Interaction Involving SPRY Domain-Containing Suppressor of Cytokine Signaling Box Protein (SPSB) 2 and Inducible Nitric Oxide Synthase

SPRY domain-containing suppressor of cytokine signaling box protein (SPSB) 2-deficient macrophages have been found to exhibit prolonged expression of inducible nitric oxide synthase (iNOS) and enhanced killing of persistent pathogens, suggesting that inhibitors of the SPSB2-iNOS interaction have potential as novel anti-infectives. In this study, we describe the design, synthesis, and characterization of cyclic peptidomimetic inhibitors of the SPSB2-iNOS interaction constrained by organic linkers to improve stability and druggability. SPR, ITC, and 19F NMR analyses revealed that the most potent cyclic peptidomimetic bound to the iNOS binding site of SPSB2 with low nanomolar affinity (KD 29 nM), a 10-fold improvement over that of the linear peptide DINNN (KD 318 nM), and showed strong inhibition of SPSB2-iNOS interaction in macrophage cell lysates. This study exemplifies a novel approach to cyclize a Type II β-turn linear peptide and provides a foundation for future development of this group of inhibitors as new anti-infectives.

AMIDE COMPOUND AND MEDICINAL USE THEREOF

A compound of formula [I-W]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.

Preparation of free and of specifically protected oligo[β-malic acids] for enzymatic degradation studies

The polyanionic poly[β-(S)-malic acids] (β-PMA) occur in slime molds (myxomycetes), black yeasts and other fungi and are involved in DNA replication. In order to be able to study the cleavage mechanism of β-PMA hydrolases, we have synthesized cyclic and linear oligomers of malic acid (β-OMA) consisting of up to eight residues. To this end, fragments with three different protecting groups were prepared, with allyl ester groups on the C-terminus, TBDPS groups at the O-terminus, and benzyl ester groups at the side chains (Schemes 2, 3, 7). Selective deprotection and fragment coupling (COCl2/C5H5N/CH2Cl2/-75 °C) gave dimers, tetramers, and octamers, either fully protected or specifically protected at the O- or C- terminus or at the side chain acid groups, and also fully deprotected oligoacids (Schemes 3-7). The new compounds were fully characterized (R(f), IR, 1H- and 13C-NMR spectroscopy, mass spectrometry and elemental analysis or high-resolution electrospray mass spectrometry). Enzymatic degradation experiments with the previously prepared cyclo-tetramer, the unprotected, and the O- or C-terminally protected samples of linear β-OMAs show that the enzyme from Physarum polycephalum is an exo-hydrolase cleaving the chain from the O-terminus.

MONOCYCLIC BETA-LACTAMS AND PROCESS FOR THE PREPARATION THEREOF

Monocyclic beta-lactam compounds represented by the formula STR1 wherein R 1 is H, NH 2, acylamino, C 1 -C 4 alkyl, etc.; R 2 is e.g. C 1 -C 4 alkyl, hydroxyalkyl, aminoalkyl, carboxy, esterified carboxy, esterified carboxyalkyl, or carboxyalkyl; and R 3 is hydrogen, benzyl, substituted benzyl, pivaloyl, --SO 3 M, or --P(C-O)(OM')2; are obtained by the cyclization of an O-substituted hydroxamate of a beta-substituted alkylcarboxylic acid. For example, alpha-ethylmalic acid monobenzyl ester is reacted with O-benzylhydroxylamine to form the O-benzylhydroxamate of the free carboxy group, and the hydroxamate is cyclized with diethyl diazodicarboxylate and triphenylphosphine to form the beta-lactam of the above formula wherein R 1 is ethyl, R 2 is benzyloxycarbonyl and R 3 is benzyl. The beta-lactam compounds are useful intermediates for preparing beta-lactamase inhibitors and monocyclic beta-lactam antibiotics and, when R 3 is --SO 3 M or -P(C-O)(OM')2 the compounds and salts thereof are antibacterial agents.