41602-50-0

Usage

InChI:InChI=1/C6H10ClNO3/c1-2-11-6(10)4-8-5(9)3-7/h2-4H2,1H3,(H,8,9)

Upstream product

• 999-29-1 N-(2-diazoacetyl)glycine ethyl ester 
• 623-33-6 glycine ethyl ester hydrochloride 
• 105-39-5 chloroacetic acid ethyl ester 
• 459-73-4 GlyOEt*HCl 
• 79-04-9 chloroacetyl chloride 
• 2087-41-4 glycyl glycine ethyl ester hydrochloride 
• 15018-06-1 chloroacetyl bromide 

Downstream Products

• 19692-13-8 4-ethoxy-7-oxo-3-oxa-5-thia-8-aza-4-phosphadecan-10-oic acid, ethyl ester, 4-sulfide 
• 34595-57-8 [2-(Ethoxy-methyl-phosphinothioylsulfanyl)-acetylamino]-acetic acid ethyl ester 
• 91695-88-4 N-(N-Cyclohexyl-glycyl)-glycin-aethylester 
• 118247-03-3 2-Acetoxy-benzoic acid (ethoxycarbonylmethyl-carbamoyl)-methyl ester 
• 289038-53-5 {2-[4-(3,3-dibutyl-7-dimethylamino-4-hydroxy-1,1-dioxo-2,3,4,5-tetrahydro-1H-1λ⁶-benzo[b]thiepin-5-yl)-phenoxy]-acetylamino}-acetic acid ethyl ester 
• 141286-93-3 N-(ethoxycarbonylmethyl)-2-(4-formylphenoxy)acetamide 
• 1073534-40-3 2-[(4-methoxyphenyl)amino]-N-(2-oxopentyl)acetamide 
• 1280669-72-8 (Z)-ethyl 2-(2-(5(4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl)acetamido)acetate 

Relevant academic research and scientific papers

Synthesis of some new 5-arylidene-2,4-thiazolidinedione esters

Compounds containing the 1,3-thiazolidine-2,4-dione scaffold are gaining increasing scientific interest as potential interventional agents for a variety of disease states. A four-step synthesis of ethyl-(2-(5-arylidine-2,4- dioxothiazolidin-3-yl)acetyl)glycinates, alaninates, butanoates, valinates and norvalinates is described. The synthesis began by converting 1,3-thiazolidine-2,4-dione into its potassium salt, which was treated with ethyl (2-chloroacetamido)glycinates, alaninates, butanoates, valinates and norvalinates, respectively, to obtain the penultimate products. These products were then subjected to a Knoevenagel condensation reaction with different aldehydes to obtain the desired products in low to excellent yields.

Discovery and evaluation of new compounds targeting ribosomal protein S1 in antibiotic-resistant Mycobacterium Tuberculosis

The emergence of antibiotic-resistant Mycobacterium Tuberculosis (Mtb) infections compels new treatment strategies, of which targeting trans-translation is promising. During the trans-translation process, the ribosomal protein S1 (RpsA) plays a key role, and the Ala438 mutant is related to pyrazinamide (PZA) resistance, which shows its effects after being hydrolysed to pyrazinoic acid (POA). In this study, based on the structure of the RpsA C-terminal domain (RpsA-CTD) and POA complex, new compounds were designed. After being synthesized, the compounds were tested in vitro with saturation transfer difference (STD), fluorescence quenching titration (FQT) and chemical shift perturbation (CSP) experiments. Finally, six of the 17 new compounds have high affinity for both RpsA-CTD and its Ala438 deletion mutant. The active compounds provide new choices for targeting trans-translation in Mtb, and the analysis of the structure-activity relationships will be helpful for further structural modifications based on derivatives of 2-((hypoxanthine-2-yl)thio)acetic acid and 2-((5-hydroxylflavone-7-yl)oxy)acetamide.

DRUGS TO TREAT OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

Derivatives and application to the asymmetric synthesis of unnatural α-amino acid derivative

We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of a-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avoided. Furthermore, using this methodology we synthesized novel a-imino carboxylic acid derivatives such as a-imino phenyl ester, perfluoroalkyl etsers, imides, and thioester. The asymmetric Mannich reaction of those novel imine derivatives with 1,3-dicarbonyl compound is also described, and the novel a-imino imide gave improved chemical yield and stereoselectivity compared with those obtained by the use of the conventional a-imino ester-type substrate.

A convenient method for preparation of α-imino carboxylic acid derivatives and application to the asymmetric synthesis of unnatural α-amino acid derivative

We describe herein a manganese(IV) oxide-mediated oxidation of N-p-methoxyphenyl (PMP)-protected glycine derivatives for the synthesis of α-imino carboxylic acid derivatives. Using this methodology, utilization of unstable glyoxic acid derivatives was avo

OXYGEN SENSOR COMPOUNDS

The invention provides the use of a luminescent heterometallic complex for detecting oxygen, which luminescent heterometallic complex comprises: a first lanthanide ion, a second lanthanide ion which is a different lanthanide from the first,and a sensitisi

New 7-methylguanine derivatives targeting the influenza polymerase PB2 cap-binding domain

The heterotrimeric influenza virus polymerase performs replication and transcription of viral RNA in the nucleus of infected cells. Transcription by "cap-snatching" requires that host-cell pre-mRNAs are bound via their 5′ cap to the PB2 subunit. Thus, the PB2 cap-binding site is potentially a good target for new antiviral drugs that will directly inhibit viral replication. Docking studies using the structure of the PB2 cap-binding domain suggested that 7-alkylguanine derivatives substituted at position N-9 and N-2 could be good candidates. Four series of 7,9-di- and 2,7,9-trialkyl guanine derivatives were synthesized and evaluated by an AlphaScreen assay in competition with a biotinylated cap analogue. Three synthesized compounds display potent in vitro activity with IC50 values lower than 10 μM. High-resolution X-ray structures of three inhibitors in complex with the H5N1 PB2 cap-binding domain confirmed the binding mode and provide detailed information for further compound optimization.

Synthesis, glucose uptake activity and structure-activity relationships of some novel glitazones incorporated with glycine, aromatic and alicyclic amine moieties via two carbon acyl linker

Three series of novel glitazones were designed and prepared by using appropriate synthetic schemes to incorporate glycine, aromatic and alicyclic amines via two carbon linker. Compounds were synthesized both under conventional and microwave methods. Nineteen out of twenty four synthesized compounds were evaluated for their in vitro glucose uptake activity using isolated rat hemi-diaphragm. Compounds, 6, 9a, 13a, 13b, 13c, 13f and 13h exhibited significant glucose uptake activity. Illustration about their synthesis and in vitro glucose uptake activity is described along with the structure-activity relationships.

Synthesis of nitrogen heterocycle-fused 1,2,4-benzothiadiazine-1,1-dioxide, quinazolinone, and pyrrolidinone derivatives with a guanidine joint via sequential aza-Wittig reaction/intramolecular NH-addition cyclization/nucleophilic substitution ring closur

We achieved efficient synthesis of imidazo- and pyrimido[1,2-b]benzo-1,2,4-thiadiazine-1,1-dioxides by the tandem aza-Wittig reaction/intramolecular NH-nucleophilic addition/NH-nucleophilic substitution cyclization methodology, involving sulfonamide ester

Synthesis of 2-, 4- And 5-(2-alkylcarbamoyl-l-methylvinyl)-7- alkyloxybenzo[b]furans and their leukotriene 64 receptor antagonistic activity

Variable benzo[6]furan derivatives having (E)- and (Z)-2-alkylcarbamoyl-l- methylvinyl groups at the 2-, 4- and 5-positions and a carboxylpropoxy or (1-phenyl)ethoxy group at the 7-position were prepared to find novel and selective leukotriene B4 (LTB4) receptor antagonists. (E)-2-(2-Diethylcarbamoyl- l-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4v) showed selective inhibition to the human BLT2 receptor (hBLT2). On the other hand, (E)-2-acetyl-4-(2-diethylcarbamoyl-l-methylvinyl)-7-(l-phenylethoxy)benzo[b] furan (7v) inhibited both human BLTi receptor (hBLT1) and hBLT 2. The (E)-2-(2-diethylcarbamoyl-l-methylvinyl) group lay on approximately the same plane as the benzo[e]furan ring, whereas the (E)-4-(2-diethylcarbamoyl-l-methylvinyl) group had the torsion angle (45.7°) from the benzo[e]furan ring plane. However, the (Z)-(2-alkylcarbamoyl-l- methylvinyl)benzo[b]furans were inactive. The inhibitory activity depended on the conformation of the 2-diethylcarbamoyl-l-methylvinyl group. The Royal Society of Chemistry 2005.