34722-37-7

Usage

InChI:InChI=1/C10H12O3S/c1-13-9-4-2-8(3-5-9)6-14-7-10(11)12/h2-5H,6-7H2,1H3,(H,11,12)

Upstream product

• 65051-28-7 1-(carboethoxy)-1-(4-methoxybenzylthio)methane 
• 824-94-2 p-methoxybenzyl chloride 
• 2746-25-0 p-Methoxybenzyl bromide 
• 68-11-1 mercaptoacetic acid 
• 6258-60-2 p-methoxybenzylmercaptan 
• 79-08-3 bromoacetic acid 
• 105-13-5 4-Methoxybenzyl alcohol 
• 79-11-8 chloroacetic acid 

Downstream Products

• 65051-29-8 2-(4-methoxybenzylmercapto)-acetohydroxamic acid 
• 136743-28-7 (4-Methoxy-benzylsulfanyl)-acetic acid 2,5-dioxo-pyrrolidin-1-yl ester 
• 28203-60-3 ((4-methoxylbenzyl)sulfonyl)acetic acid 
• 28203-55-6 ((4-methoxybenzyl)sulfinyl)acetic acid 
• 858104-45-7 (4S)-3-{2-[(4-methoxyphenyl)methylthio]acetyl}-4-phenyl-1,3-oxazolidin-2-one 
• 34722-44-6 methyl 2-((4-methoxybenzyl)thio)acetate 
• 917887-11-7 tert-butyl (4-{(2R,3R)-1-(4-chlorophenyl)-3-[(4-methoxybenzyl)thio]-4-oxoazetidin-2-yl}phenoxy)acetate 
• 858104-46-8 tert-butyl (4-{(1R)-1-[(4-fluorophenyl)amino]-2-[(4-methoxybenzyl)thio]-3-oxo-3-[(4S)-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]propyl}phenoxy)acetate 
• 858104-47-9 (3R,4R)-1-(4-fluorophenyl)-3-(4-methoxybenzylsulphanyl)-4-[4-(t-butoxycarbonylmethoxy)phenyl]azetidin-2-one 
• 1609008-06-1 E-acetic acid 2-acetoxy-4-[2-(4-methoxyphenylmethanesulfinyl)vinyl]phenyl ester 
• 1609007-98-8 E-acetic acid 2-acetoxy-4-[2-(4-methoxyphenylmethanesulfonyl)vinyl]phenyl ester 
• 592542-51-3 4-methoxy-3-nitrophenylmethanesulfonyl acetic acid 
• 1011290-96-2 1-(2-(4-methoxybenzylthio)acetyl)-2-methyl-3-phenylisothiourea 
• 1011291-07-8 dimethyl [2-((4-methoxybenzyl)thio)acetyl]carbonodithioimidate 

Relevant academic research and scientific papers

Styryl sulfones compound, its preparation method and its use as neuroprotective agents

The application relates to design of a novel molecule with ester group substituted by sulfone group by using a caffeic acid phenethyl ester (CAPE) with neuroprotective activity extracted from natural propolis as a primer according to bioisosterism principle and hydrogen-bond interaction theory; and the molecule has a structural general formula I, and the definition of each group is shown in the claims. The invention also relates to compound in vitroantioxidation capability evaluation, neuroprotective activity evaluation on cell level and traverse blood brain barrier ability evaluation. Activity evaluation results show that the synthesized novel compound has enhanced neuroprotective activity and can easily traverse the blood brain barrier, thus becoming a novel neuroprotective agent for treating neurodegenerative diseases.

Substituted α-mercaptoketones, new types of specific neprilysin inhibitors

New neprilysin inhibitors containing an α-mercaptoketone HSC(R1R2)CO group, as zinc ligand were designed. Two parameters were explored for potency optimization: the size of the inhibitor which could interact with the S1, S

E-3,4-di-calcium method for preparing vinyl sulfoxide compound thereof as a neuroprotective pharmaceutical application

The invention relates to an application of E-3,4-dihydroxyphenylvinyl sulfoxide represented by the formula I in preparation of nerve protection drugs for treating neurodegenerative diseases, wherein the definitions of each group in the formula I are listed in the description. The invention also relates to a preparation method of E-3,4-dihydroxyphenylvinyl sulfoxide.

MIXED INHIBITORS OF AMINOPEPTIDASE N AND NEPRILYSIN

Mixed inhibitors of aminopeptidase N and neprilysin are disclosed. Pharmaceutical compositions containing at least one of these compounds, used alone or in combination with morphine and derivatives thereof, endocannabinoids and inhibitors of endocannabinoid metabolism, GABA derivatives such as gabapentin or pregabalin, duloxetine or methadone, can be used as an analgesic, anxiolytic, antidepressant or anti-inflammatory.

Design, synthesis, and biological evaluation of (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides as novel multifunctional neuroprotective agents

Novel (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides were designed and synthesized as new analogues of 1, which showed interesting multifunctional neuroprotective effects, including antioxidative and antineuroinflammatory properties. Specifically, target compounds display excellent potency in scavenging reactive free radicals and demonstrate potent effects against various kinds of toxicities, including H2O2, 6-hydroxydopamine, and lipopolysaccharide in different types of neuronal cells. The antioxidative properties of the target compounds are more potent than that of 1, and the antineuroinflammatory properties are less strong than that of 1. According to the parallel artificial membrane permeation assay for the blood-brain barrier, target compounds possess greater blood-brain barrier (BBB) permeability than 1. In short, due to improvement of the antioxidative effect, stability, and BBB permeability, (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides can thus be considered as potential multifunctional neuroprotective agents and serve as new lead candidates in the treatment of neurodegenerative diseases.

Synthesis and antioxidant activity of 1,4-[Bis(3-arylmethanesulfonyl pyrrolyl and pyrazolyl)]benzenes

A variety of (1,4-phenylene)bis(arylmethanesulfonylpyrroles and pyrazoles) were prepared by the cycloaddition of 1,3-dipolar reagents, tosylmethyl isocyanide and diazomethane to the Michael acceptor, 1,4-bis(E)-2- ((arylmethanesulfonyl)vinyl)benzene. All the compounds were evaluated for antioxidant activity. Amongst the tested compounds, one of them displayed excellent radical scavenging activity in all the three methods evaluated when compared with the standard Ascorbic acid. On the other hand, 1,4-(bis(3-arylmethanesulfonyl)-1H-pyrazol-4-yl)benzenes exhibited comparatively higher antioxidant activity than 1,4-(bis(3-arylmethanesulfonyl)-1H-pyrrol-4- yl) benzenes. In general, it was observed that compounds having methoxy substitutent on aromatic ring displayed greater antioxidant activity than the other substituents. ?2014 Sociedade Brasileira de Qui?mica.

Design, synthesis, and biological evaluation of (E)-styrylbenzylsulfones as novel anticancer agents

Cell cycle progression is regulated by cyclins and cyclin-dependent kinases, which are formed at specific stages of the cell cycle and regulate the G1/S and G2/M phase transitions, employing a series of "checkpoints" governed by phosphorylation of their substrates. Tumor development is associated with the loss of these checkpoint controls, and this provides an approach for the development of therapeutic agents that can specifically target tumor cells. Here, we describe the synthesis and SAR of a novel group of cytotoxic molecules that selectively induce growth arrest of normal cells in the G1 phase while inducing a mitotic arrest of tumor cells resulting in selective killing of tumor cell populations with little or no effect on normal cell viability. The broad spectrum of antitumor activity in vitro and xenograft models, lack of in vivo toxicity, and drug resistance suggest potential for use of these agents in cancer therapy.

ALPHA, BETA-UNSATURATED SULFOXIDES FOR TREATING PROLIFERATIVE DISORDERS

alphabeta-Unsaturated sulfoxides of Formula I: (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Comparison of the labelling characteristics of mercaptoacetyltriglycine (MAG3) with different S-protective groups

A number of different thiol protective groups have been synthesized and attached to mercaptoacetyltriglycine (MAG3) ligand. The newly made MAG3 analogues were labelled with 99mTc by direct labelling under alkaline condition and by stannous tartrate exchange labelling method. In the latter method, the amount of the ligand, reaction temperature and pH varied and their effects on the labelling efficiencies were studied. Radiochemical purities of 51% to 70%, 58% to 75% and 46% to 81% respectively, were obtained by radio-HPLC analysis for the studied MAG3 precursors when, 0.1 mg, 0.4 mg and 1.6 mg of the ligand was used and labelling was performed at both low temperature (70°C) and pH (pH 3). All the studied ligands were efficiently labelled with 99mTc (up to 99%) when heated for 10 min at pH 9 and 100°C. The labelling efficiency obtained by the direct labelling method for MAG3 analogues varied from 32% to 94% and was in all cases lower than after the exchange labelling at pH 9 and at 100°C. It was observed that the radiochemical purities can be improved significantly by heating the 'direct labelling mixture' at elevated temperature.

Phenylamidine derivatives

A compound having the general formula: STR1 wherein Ar is an aryl group (especially an α-naphthyl, β-naphthyl or phenyl group) which may be substituted by one or more C1-4 alkyl, C1-4 alkoxy, methylenedioxy halogen, CF3, NH2 or NO2 groups; A is a --CH2 --, --CHOH--, --CH2 O--, --CH2 S--, --CH2 NH--, --OCH2 --, --SCH2 --, --NH--, --NHCOCH2 --, --CH2 NHCH2 -- or --NHCH2 -- group; Y is O or NH; and B is a single bond and, when A is --CH2 --S, may be a --CH2 --, or --CH(CH3)-- group; and their acid addition salts when Y is NH and their metal salts when Y is O. The compounds and their salts have therapeutic utility in treatment of neuropsychic ailments.