cas 5330-71-2, Benzoic acid, 4-[[(phenylmethoxy)carbonyl]amino]- (9CI)

Articles about 5330-71-2Total 10 be found

CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF
Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
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(2019/04/05)

Synthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis
A series of novel hydrogen peroxide sensitive prodrugs of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in mice with collagen induced arthritis (CIA) as a model of chronic rheumatoid arthritis (RA). The prodrug strategy selected is based on ROS-labile 4-methylphenylboronic acid promoieties linked to the drugs via a carbamate linkage or a direct C-N bond. Activation under pathophysiological concentrations of H2O2 proved to be effective, and prodrug candidates were selected in agreement with relevant in vitro physicochemical and pharmacokinetic assays. Selected candidates showed moderate to good solubility, high chemical and enzymatic stability, and therapeutic efficacy comparable to the parent drugs in the CIA model. Importantly, the prodrugs displayed the expected safer toxicity profile and increased therapeutic window compared to MTX and AMT while maintaining a comparable therapeutic efficacy, which is highly encouraging for future use in RA patients.
Peiró Cadahía, Jorge,Bondebjerg, Jon,Hansen, Christian A.,Previtali, Viola,Hansen, Anders E.,Andresen, Thomas L.,Clausen, Mads H.
p. 3503 - 3515
(2018/05/01)

PRODRUGS ACTIVATED BY REACTIVE OXYGEN SPECIES FOR USE IN THE TREATMENT OF INFLAMMATORY DISEASES AND CANCER
Prodrugs activated predominantly or exclusively in inflammatory tissue, more particularly prodrugs of methotrexate and derivatives thereof, which are selectively activated by Reactive Oxygen Species (ROS) in inflammatory tissues associated with cancer and inflammatory diseases, as well as method for preparing said prodrugs.
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(2018/09/25)

Optimization of amino acid thioesters as inhibitors of metallo-β-lactamase L1
The emergence of antibiotic resistance caused by metallo-β-lactamases (MβLs) is a global public health problem. Recently, we found amino acid thioesters to be a highly promising scaffold for inhibitors of the MβL L1. In order to optimize this series of inhibitors, nine new amino acid thioesters were developed by modifying the substituents on the N-terminus of the thioesters and the groups representing the amino acid side chain. Biological activity assays indicate that all of them are very potent inhibitors of L1 with an IC50value range of 20–600?nM, lower than those of most of the previously reported inhibitors of this scaffold. Analysis of structure–activity relationship reveals that big hydrophobic substituents on the N-terminus and a methionine amino acid side chain improves inhibitory activity of the thioesters. All these inhibitors are able to restore antibacterial activity of a β-lactam antibiotic against Escherichia coli BL21(DE3) cells producing L1 to that against E. coli cells lacking a β-lactamase. Docking studies reveal that a large N-terminal hydrophobic group results in a slightly different binding mode than smaller hydrophobic groups at the same position.
Liu, Xiao-Long,Yang, Ke-Wu,Zhang, Yue-Juan,Ge, Ying,Xiang, Yang,Chang, Ya-Nan,Oelschlaeger, Peter
p. 4698 - 4701
(2016/09/13)

Highly potent and selective fluorescent antagonists of the human adenosine A3 receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold
The adenosine-A3 receptor (A3AR) is a G protein-coupled receptor that shows promise as a therapeutic target for cancer, glaucoma, and various autoimmune inflammatory disorders, and as such, there is a need for molecular probes to study this receptor. Here, we report a series of fluorescent ligands containing different linkers and fluorophores based around a 1,2,4-triazolo[4,3-a]quinoxalin-1-one antagonist. One of these conjugates (19) displayed high affinity for the A3AR (pKD = 9.36 ± 0.12) and is >650-fold selective over other adenosine receptor subtypes. Confocal microscopy revealed clear, displaceable membrane labeling of CHO-A 3 cells with 19, with no detectable labeling of CHO-A1 cells under identical conditions. This fluorescent ligand was also able to specifically label the A3AR in HEK293T cells containing a mixed adenosine receptor population. The subtype specificity, along with its excellent imaging properties, make 19 an ideal tool for studying A3AR distribution and organization, particularly in the presence of other adenosine receptor subtypes.
Vernall, Andrea J.,Stoddart, Leigh A.,Briddon, Stephen J.,Hill, Stephen J.,Kellam, Barrie
experimental part
p. 1771 - 1782
(2012/05/04)

Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins
The tenovins are small molecule inhibitors of the NAD+-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neuro
McCarthy, Anna R.,Pirrie, Lisa,Hollick, Jonathan J.,Ronseaux, Sebastien,Campbell, Johanna,Higgins, Maureen,Staples, Oliver D.,Tran, Fanny,Slawin, Alexandra M.Z.,Lain, Sonia,Westwood, Nicholas J.
scheme or table
p. 1779 - 1793
(2012/04/17)

SURFACE-MODIFIED POLYMER FILMS
Surface-modified polymer films for coating are provided, wherein the surface is modified by covalent binding of nano- or micro-particles comprising a photoreactive species. The surface of the polymer film, e.g. a parylene film, may be modified by covalent
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(2013/03/26)

A catalyst-free N-benzyloxycarbonylation of amines in aqueous micellar media at room temperature
N-Benzyloxycarbonylation of amines was carried out in aqueous micellar media. Aliphatic (open and cyclic), aromatic and heteroaromatic amines react with Cbz-Cl to give excellent yields of products. The reactions were carried out in water and at room temperature.
Shrikhande, Janhavi J.,Gawande, Manoj B.,Jayaram, Radha V.
p. 4799 - 4803
(2008/12/22)

Aqueous phase mono-protection of amines and amino acids as N-benzyloxycarbonyl derivatives in the presence of β-cyclodextrin
A simple and selective protection of amines/amino acids with Cbz-Cl has been achieved in aqueous phase with catalytic amounts of β-cyclodextrin in high yields at room temperature. This reaction proceeds without the formation of any by-products and has advantages over existing methods.
Pavan Kumar,Somi Reddy,Narender,Surendra,Nageswar,Rama Rao
p. 6393 - 6396
(2007/10/03)

Highly chemoselective hydrogenation method using novel finely dispersed palladium catalyst on silk-fibroin: Its preparation and activity
A palladium-fibroin complex (Pd/Fib) was prepared by soaking silk-fibroin in MeOH solution of Pd(OAc)2 for 2 days (under Ar atmosphere) - 4 days (under air). Pd(OAc)2 was gradually absorbed by fibroin and the rapid reduction of fibroin conjugated Pd(OAc)2 proceeded with MeOH as a reductant at room temperature to be the Pd(0) complex. Pd/Fib catalyzed chemoselective hydrogenation of acetylenes, olefins and azides in the presence of aromatic ketones and aldehydes, halides, N-Cbz protective groups and benzyl esters which are readily hydrogenated using Pd/C or Pd/C(en) as a catalyst.
Ikawa, Takashi,Sajiki, Hironao,Hirota, Kosaku
p. 2217 - 2231
(2007/10/03)