37167-62-7Relevant academic research and scientific papers
NEGATIVE ALLOSTERIC MODULATION OF GLUN3-CONTAINING N-METHYL-D-ASPARTATE RECEPTORS
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Page/Page column 65, (2021/08/06)
Disclosed are negative allosteric modulators of GluN3-containing NMDA receptors. In general, these compounds are highly selective for GluN3 (such as GluN3A and/or GluN3B) over GluN1 and/or GluN2. They can function as non-competitive antagonists with activity that is independent of membrane potential, glycine concentration, and extracellular pH. Also disclosed are pharmaceutical formulations of the negative allosteric modulators. These compounds can be used to enhance synaptic function and/or treating a neurological condition or disorder. Exemplary neurological conditions or disorders include, but are not limited to, major mental disorders, conditions that involve basal ganglia or altered dopamine, substance abuse/addiction or predisposition to substance abuse/addiction, pain disorders, developmental delay or situations with impaired learning, memory, and/or cognition, acute neuronal or glial injuries, and circuit disorders.
Manganese/bipyridine-catalyzed non-directed C(sp3)–H bromination using NBS and TMSN3
Sneh, Kumar,Torigoe, Takeru,Kuninobu, Yoichiro
supporting information, p. 885 - 890 (2021/05/05)
A Mn(II)/bipyridine-catalyzed bromination reaction of unactivated aliphatic C(sp3)?H bonds has been developed using N-bromosuccinimide (NBS) as the brominating reagent. The reaction proceeded in moderate-to-good yield, even on a gram scale. The introduced bromine atom can be converted into fluorine and allyl groups.
MALIC ENZYME INHIBITORS
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, (2021/04/23)
The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans.
Activating ATRP Initiators to Incorporate End-Group Modularity into Photo-RAFT Polymerization
Hakobyan, Karen,McErlean, Christopher S. P.,Müllner, Markus
, p. 10357 - 10365 (2020/12/23)
Heterogeneous photocatalysis is increasingly used in reversible deactivation radical polymerization (RDRP). In this study, we found that alkyl bromide redox chemistry typically found in atom transfer radical polymerization (ATRP) can be incorporated in concert with dithiocarbonyl disulfide chemistry into the reversible addition-fragmentation chain transfer (RAFT) process via bismuth oxide photocatalysis. This amalgamation of mechanisms introduces end-group modularity - a new layer of control - into RAFT polymers uniquely enabled by photoredox catalysis. We found that a diversity of functionality can be installed at the α-end group via alkyl bromides, while the molecular weight distribution can be tuned seamlessly at the ω-end group through the simultaneous addition of multiple disulfides.
Bromination of α-Diazo Phenylacetate Derivatives Using Cobalt(II) Bromide
Wang, Haifeng,Sun, Xiangli,Hu, Manman,Zhang, Xiaoyi,Xie, Lele,Gu, Shuangxi
supporting information, p. 3347 - 3351 (2020/07/04)
A method for the bromination of α-diazo phenylacetate derivatives using cobalt(II) bromide is described. This bromination reaction features a short reaction time, broad substrate scope, operational simplicity, acid-free conditions, and gram-scalability. (Figure presented.).
Synthesis and biological evaluation of 3-functionalized 2-phenyl- and 2-alkylbenzo[b]furans as antiproliferative agents against human melanoma cell line
Kwiecień, Halina,Peru?yńska, Magdalena,Stachowicz, Karolina,Piotrowska, Katarzyna,Bujak, Joanna,Kopytko, Patrycja,Dro?dzik, Marek
supporting information, (2019/04/29)
The key function of microtubules and mitotic spindle in cell division make them attractive targets in anticancer therapy. In the present study, functionalized in 3 position 2-phenyl- and 2-alkylbenzo[b]furans were synthesized and evaluated as antitumor ag
Visible Light-Mediated Conversion of Alcohols to Bromides by a Benzothiadiazole-Containing Organic Photocatalyst
Li, Run,Gehrig, Dominik W.,Ramanan, Charusheela,Blom, Paul W. M.,Kohl, Fabien F.,Wagner, Manfred,Landfester, Katharina,Zhang, Kai A. I.
, p. 3852 - 3859 (2019/07/15)
The search for metal-free, stable and high effective photocatalysts with sufficient photo-redox potentials remains a key challenge for organic chemists. Here, we present a benzothiadiazole-containing molecular organic photocatalyst with redox potentials of ?1.30 V and +1.64 V vs. SCE. The singlet state lifetime is 13 ns. Direct conversion from aliphatic alcohols to bromides has been conducted with the designed organic photocatalyst under visible light irradiation with high efficiency and selectivity. The catalytic efficiency of the novel benzothiadiazole-based photocatalyst is comparable with the state-of-art metal and non-metal catalysts. Furthermore, advanced photophysical studies including time-resolved photoluminescence and transient absorption spectroscopy offer a powerful support for photo-induced electron transfer from photocatalyst to the reactive substrates. Lastly, no photo-bleaching effect is observed, demonstrating the high stability and recyclable of the designed organic photocatalyst. (Figure presented.).
New 4-aryl-1,3,2-oxathiazolylium-5-olates: Chemical synthesis and photochemical stability of a novel series of S-nitrosothiols
Eilertsen, Monica,Allin, Steve M.,Pearson, Russell J.
supporting information, p. 1106 - 1110 (2018/02/28)
S-nitrosothiols (RSNOs) remain one of the most popular classes of NO-donating compounds due to their ability to release nitric oxide (NO) under non-enzymatic means whilst producing an inert disulphide by-product. However, alligning these compounds to the different biological fields of NO research has proved to be problematic due to the inherent instability of such compounds under a variety of conditions including heat, light and the presence of copper ions. 1,3,2-Oxathiazolylium-5-olates (OZOs) represent an interesting subclass of S-nitrosothiols that lock the –SNO moiety into a five membered heterocyclic ring in an attempt to improve the compound's overall stability. The synthesis of a novel series of halogen-containing OZOs was comprehensively studied resulting in a seven-step route and overall yields ranging between 21 and 37%. The photochemical stability of these compounds was assessed to determine if S-nitrosothiols locked within these mesoionic ring systems can offer greater stability and thereby release NO in a more controllable fashion than their non-cyclic counterparts.
Mandelic acid derived ionic liquids: synthesis, toxicity and biodegradability
Prydderch, Hannah,Haiβ, Annette,Spulak, Marcel,Quilty, Brid,Kümmerer, Klaus,Heise, Andreas,Gathergood, Nicholas
, p. 2115 - 2126 (2017/01/22)
A series of ten ionic liquids (ILs) was synthesised from the renewable resource mandelic acid. The ILs showed low antimicrobial activity towards the thirteen bacterial and twelve fungal strains they were screened against. A general trend of increasing bacterial toxicity in the order methyl ester 60% in 28 days), a series of biodegradation transformation products has been proposed based on the degradation of the ester/amide alkyl chain. This data has allowed for an assessment of the effect of IL structural features on toxicity and biodegradation, particularly allowing for a comparison to earlier work where additional oxygen atoms were present to facilitate biodegradation and attenuate toxicity. The mandelic acid derived ILs did not pass the Closed Bottle test (OECD 301D) and can be included in the rules of thumb for the design of biodegradable ILs.
Synthesis and PGE2 production inhibition of s-triazine derivatives as a novel scaffold in RAW 264.7 macrophage cells
Kang, Seoung Mook,Lee, Jinsung,Jin, Jae Ho,Kim, Minju,Lee, Sunhoe,Lee, Hwi Ho,Shin, Ji-Sun,Lee, Kyung-Tae,Lee, Jae Yeol
, p. 5418 - 5422 (2015/01/08)
We present the synthesis and biological evaluation of a collection of s-triazine derivatives as a novel scaffold of compounds with the capability to inhibit the PGE2 production in LPS-induced RAW 264.7 macrophage cells. A total of 12 derivatives were synthesized and assayed for PGE2 reduction at 10 μM concentration. Two compounds (7b and 7i) exhibiting >90% inhibition of PGE2 production were found to have IC50 values of 5.76 and 5.52 μM, respectively. They were counter screened for inhibition on COX-2 activity in a cell free assay. Specifically, compound 7i (R1 = 4-Bn-Ph, R2 = Cl, R3 = Ph, R5 = CO2Me) was highly active in cells while maintaining little COX-2 inhibition (~0% at 10 μM). Molecular docking study provides the possibility that compound 7i could inhibit PGE2 production by blocking the PGH2 binding site of mPGES-1 instead of COX-2 enzyme. Based on this result, our synthetic efforts will focus on intensive structure-activity relationship (SAR) study of s-triazine scaffold to discovery a potential PGE2 synthesis inhibitor.
