Tag: M.W=200-250

Padmanabhan, Seetharamaiyer; Lavin, Ruth C.; Thakker, Paresh M.; Guo, Jinqing; Zhang, Lu; Moore, Deke; Perlman, Michael E.; Kirk, Cassandra; Daly, Deborah; Burke-Howie, Kathy J.; Wolcott, Teresa; Chari, Suchitra; Berlove, David; Fischer, James B.; Holt, William F.; Durant, Graham J.; McBurney, Robert N. published the artcile< Solution-Phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers>, HPLC of Formula: 2905-54-6, the main research area is acylguanidine synthesis sodium channel blocker human cardiac.

Solution-phase synthesis of various acylguanidine derivatives and the evaluation of a small library of compounds as potential sodium channel blockers are described.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 2905-54-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6Cl2O2, HPLC of Formula: 2905-54-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rajak, Harish; Agarawal, Avantika; Parmar, Poonam; Thakur, Bhupendra Singh; Veerasamy, Ravichandran; Sharma, Prabodh Chander; Kharya, Murli Dhar published the artcile< 2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: Design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors>, Formula: C8H6ClN3S, the main research area is tetrahydropyranyloxy aryloxadiazolecarboxamide arylthiadiazolecarboxamide preparation histone deacetylase inhibitor antitumor.

The enzymic inhibition of histone deacetylase activity has come out as a novel and effectual means for the treatment of cancer. Two novel series of 2-[5-(4-substituted phenyl)-[1,3,4]-oxadiazol- and -thiadiazol-2-ylamino]pyrimidine-5-carboxylic acid (tetrahydropyran-2-yloxy)amides were designed and synthesized as novel hydroxamic acid based histone deacetylase inhibitors. The antiproliferative activities of the compounds were investigated in vitro using histone deacetylase inhibitory assay and MTT assay. The synthesized compounds were also tested for antitumor activity against Ehrlich ascites carcinoma cells in Swiss albino mice. Efforts were also made to establish structure-activity relationships among synthesized compounds The results of the present study indicate that these compounds are promising surface recognition moieties for development of newer hydroxamic acid based histone deacetylase inhibitor.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Formula: C8H6ClN3S.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jiao, Ke-Jin; Ma, Cong; Liu, Dong; Qiu, Hui; Cheng, Bin; Mei, Tian-Sheng published the artcile< Nickel-catalyzed electrochemical reductive relay cross-coupling of alkyl halides with alkyl carboxylic acids>, Application of C8H8BrCl, the main research area is alkyl acid bromoalkane nickel regioselective electrochem reductive cross coupling; dialkyl ketone preparation.

A highly regioselective Ni-catalyzed electrochem. (undivided cell) reductive relay cross-coupling between alkyl carboxylic acids and alkyl bromides was developed. This strategy allowed the direct acylation of benzylic C(sp3)-H bonds in good yields from com. available alkyl carboxylic acids, thus provided an alternative strategy for the synthesis of dialkyl ketones. Various functional groups were tolerated under mild reaction conditions.

Organic Chemistry Frontiers published new progress about Acylation catalysts (regioselective, electrochem.). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Application of C8H8BrCl.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Guan, Peng; Wang, Lei; Hou, Xuben; Wan, Yichao; Xu, Wenfang; Tang, Weiping; Fang, Hao published the artcile< Improved antiproliferative activity of 1,3,4-thiadiazole-containing histone deacetylase (HDAC) inhibitors by introduction of the heteroaromatic surface recognition motif>, Quality Control of 70057-67-9, the main research area is antiproliferative thiadiazole preparation histone deacetylase inhibitor structure activity modeling; 1,3,4-Thiadiazole; Antiproliferation; Histone deacetylase inhibitor; Hydroxamic acid; Surface recognition motif.

A series of 1,3,4-thiadiazole-containing hydroxamic acids, in accord with the common pharmacophore of histone deacetylase (HDAC) inhibitors (a Zn2+ binding moiety-a linker-a surface recognition motif), was identified as submicromolar HDAC inhibitors by the authors’ group. In this study, the authors continued the efforts to develop 1,3,4-thiadiazole bearing hydroxamate analogs by modifying the surface recognition motif. The authors found that 1,3,4-thiadiazoles having a heteroaromatic substituent showed better HDAC inhibitory activity in enzymic assay and higher antiproliferative potency in cellular assay compared to SAHA.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Quality Control of 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Dockendorff, Chris; Aisiku, Omozuanvbo; VerPlank, Lynn; Dilks, James R.; Smith, Daniel A.; Gunnink, Susanna F.; Dowal, Louisa; Negri, Joseph; Palmer, Michelle; MacPherson, Lawrence; Schreiber, Stuart L.; Flaumenhaft, Robert published the artcile< Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor>, Category: chlorides-buliding-blocks, the main research area is preparation of antithrombotic agent platelet activation inhibition PAR1.

A high-throughput screen of the NIH-MLSMR compound collection, along with a series of secondary assays to identify potential targets of hit compounds, previously identified a 1,3-diaminobenzene scaffold that targets protease-activated receptor 1 (PAR1). We now report addnl. structure-activity relationship (SAR) studies that delineate the requirements for activity at PAR1 and identify plasma-stable analogs with nanomolar inhibition of PAR1-mediated platelet activation. Compound 4 was declared as a probe (ML161) with the NIH Mol. Libraries Program. This compound inhibited platelet aggregation induced by a PAR1 peptide agonist or by thrombin but not by several other platelet agonists. Initial studies suggest that ML161 is an allosteric inhibitor of PAR1. These findings may be important for the discovery of antithrombotics with an improved safety profile.

ACS Medicinal Chemistry Letters published new progress about Anticoagulants. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Liu, Zheng; Bian, Ming; Ma, Qian-Qian; Zhang, Zhuo; Du, Huan-Huan; Wei, Cheng-Xi published the artcile< Design and synthesis of new benzo[d]oxazole-based derivatives and their neuroprotective effects on β-amyloid-induced PC12 cells>, HPLC of Formula: 70057-67-9, the main research area is benzoxazolylthio aryl thiadiazolyl acetamide preparation Alzheimer neuroprotective amyloid; Akt/GSK-3β/NF-κB signaling pathway; Alzheimer’s disease; benzo[d]oxazol; synthesis; thiadiazoles; β-amyloid.

A series of novel synthetic substituted benzo[d]oxazole-based derivatives I (R = H, 3,4,5-(OMe)3, 2-Cl-5-F, etc.) exerted neuroprotective effects on β-amyloid (Aβ)-induced PC12 cells as a potential approach for the treatment of Alzheimer’s disease (AD). In vitro studies show that most of the synthesized compounds I were potent in reducing the neurotoxicity of Aβ25-35-induced PC12 cells at 5μg/mL. The compound I (R = 3-Cl) (II) was non-neurotoxic at 30μg/mL and significantly increased the viability of Aβ25-35-induced PC12 cells at 1.25, 2.5 and 5μg/mL. Western blot anal. showed that compound II promoted the phosphorylation of Akt and glycogen synthase kinase (GSK-3β) and decreased the expression of nuclear factor-κB (NF-κB) in Aβ25-35-induced PC12 cells. In addition, the findings demonstrated that compound II protected PC12 cells from Aβ25-35-induced apoptosis, reduced the hyperphosphorylation of tau protein, and decreased the expression of receptor for AGE (RAGE), β-site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1), inducible nitric oxide synthase (iNOS) and Bcl-2-associated X protein/B-cell lymphoma 2 (Bax/Bcl-2) via Akt/GSK-3β/NF-κB signaling pathway. In vivo studies suggest that compound II shows less toxicity than donepezil in the heart and nervous system of zebrafish.

Molecules published new progress about Alzheimer disease. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, HPLC of Formula: 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Calas, Michele; Ouattara, Mahama; Piquet, Gilles; Ziora, Zyta; Bordat, Y.; Ancelin, Marie L.; Escale, Roger; Vial, Henri published the artcile< Potent Antimalarial Activity of 2-Aminopyridinium Salts, Amidines, and Guanidines>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is aminopyridinium salt amidine guanidine derivative preparation antimalarial malaria Plasmodium.

The authors describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10-6-10-7 M concentration range. IC50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC50 < 10 nM). Increasing the alkyl chain length from 6 to 12 methylene groups led to increased activity, while beyond this antimalarial activity decreased. Antimalarial activities appear to be strictly related to the basicity of the cationic head with an optimal pKa over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely addnl. binding opportunities on account of their hydrogen-bond-forming properties. Journal of Medicinal Chemistry published new progress about Antimalarials. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Liao, Ke; Wu, Fengjin; Chen, Jiean; Huang, Yong published the artcile< Catalytic cleavage and functionalization of bulky and inert Csp3-Csp3 bonds via a relayed proton-coupled electron transfer strategy>, COA of Formula: C6H4Cl2N4, the main research area is alc radicalophile acridinium tetrafluoroborate regioselective photochem bond cleavage functionalization.

The direct, photoredox cleavage of hindered Csp3-Csp3 bonds of alcs. under neutral conditions was described. A relayed proton-coupled electron transfer (PCET) strategy was employed that overcame the previous requirement of a Bronsted base. Heavily branched alcs. with a high oxidation potential (Eox1/2 > +2 V vs. SCE) were cleaved and functionalized with remarkable efficiency and versatility. A simple, non-substituted Ph group can promote a relayed PCET process to deliver primary, secondary, and tertiary alkyl radicals under neutral conditions.

Cell Reports Physical Science published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, COA of Formula: C6H4Cl2N4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wang, Zian; Yao, Jingwen; Zhan, Lisi; Gong, Shaolong; Ma, Dongge; Yang, Chuluo published the artcile< Purine-based thermally activated delayed fluorescence emitters for efficient organic light-emitting diodes>, SDS of cas: 2382-10-7, the main research area is purine derivative thermally activated delayed fluorescence organic LED; diode light emitting organic purine derivative thermal delayed fluorescence; electroluminescent device organic purine derivative thermally activated delayed fluorescence.

Two thermally-activated delayed fluorescence (TADF) emitters (1PXZP and 2PXZP) based on a novel biol. base acceptor of 9-methylpurine and commonly used donor of phenoxazine (PXZ) were synthesized and characterized. Both target compounds possess nearly orthogonal configurations to reduce singlet-triplet splitting energy (ΔEST) for remarkable TADF character. The 2 emitters show good luminescence quantum yields (PLQYs), and the organic LEDs employing 1PXZP and 2PXZP as emitters display good performance with maximum external quantum efficiencies of 10.6 and 13.8%, resp. The efficiencies of 1PXZP based device show nearly no roll-off at 100 cd m-2 luminance due to the short delayed lifetime (τd) of 3.2μs. This work manifests that the biol. base is a promising acceptor for designing TADF materials.

Dyes and Pigments published new progress about Cyclic voltammetry. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, SDS of cas: 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tan, Zhenda; Ci, Chenggang; Yang, Jian; Wu, Yang; Cao, Liang; Jiang, Huanfeng; Zhang, Min published the artcile< Catalytic Conversion of N-Heteroaromatics to Functionalized Arylamines by Merging Hydrogen Transfer and Selective Coupling>, Reference of 320407-92-9, the main research area is azaarene alkyl bromide amino arylmethanol ruthenium hydrogen transfer coupling; alkylaminoaryl methylazaarene preparation chemoselective.

A ruthenium-catalyzed deconstruction of N-heteroaromatics to functionalized arylamines with 2-aminoaryl methanols via hydrogen transfer and selective coupling was reported. The reaction was achieved via sequential functionalization of the β and α-sites of the initially formed N-heteroarenium salts followed by a C-N cleavage, proceeding with the striking features of broad substrate scope, excellent functional groups tolerance, high chemoselectivity and atom-efficiency, and applicable for streamline synthesis of some biomedical mols. The strategy utilized will pave the avenues for further development of catalytic transformations of inert organo-systems to functional frameworks.

ACS Catalysis published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 320407-92-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrClO, Reference of 320407-92-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics