Tag: M.W=150-200

Al-Rubaie, Ali Z. published the artcilePalladium-catalyzed formation of 3,5-diaryl-1,2,4-selenadiazoles from arylselenocarboxamide, COA of Formula: C9H9NO2, the main research area is diarylselenadiazole preparation; arylselenocarboxamide preparation cyclization; selenadiazole diaryl preparation.

A number of new and known arylselenocarboxamides RC(:Se)NH2 [R = Ph, 4-BrC6H4, 2-MeOC6H4, 4-MeOC6H4, 4-MeSC6H4, 4-EtOC6H4, 2,3-(MeO)2C6H3, 3,4-(MeO)2C6H3, 3,5-(MeO)2C6H3, 4-PhC6H4, 6-MeOC10H6, 4-MeOC10H6] have been prepared in high yields by the reaction of RCN with NaHSe. Treatment of RC(:Se)NH2 (4 mmol) with aqueous Na2PdCl4 (1 mmol) in acetone at room temperature resulted in the formation of 3,5-diaryl-1,2,4-selenadiazoles (L) as unexpected products together with palladium(II) complexes [PdCl2L]2.2H2O. Treatment of RC(:Se)NH2 (4 mmol) with catalytic amounts of Na2PdCl4 (10-3 mmol) gave only 3,5-diaryl-1,2,4-selenadiazoles in good yields. 3,5-Diaryl-1,2,4-selenodiazoles were also prepared by oxidation of arylselenocarboxamides with iodine for comparison.

Journal of Organometallic Chemistry published new progress about diarylselenadiazole preparation; arylselenocarboxamide preparation cyclization; selenadiazole diaryl preparation. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, COA of Formula: C9H9NO2.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Jie, Zhou published the artcileDiethyl Chlorophosphite: A Versatile Reagent, Recommanded Product: 2,3-Dimethoxybenzonitrile, the main research area is diethyl chlorophosphite reaction oxygenated functional group.

Di-Et chlorophosphite (DECP) was previously described as a reducing agent for nitro compounds to amines (B. Fischer and L. Sheihet, J. Organic Chem. 1998, 63, 393). Here, the utility of this reagent was extended to chem. conversions of other oxygenated functional groups. In this paper we report on the scope of the reaction of DECP with N-oxides, epoxides, sulfones, sulfoxides, hydroxylamines, ketoximes, and aldoximes. The chemoselectivity of DECP is described, and conditions for a stepwise multiple conversion of functional groups on the same mol. with this reagent are provided.

Journal of Organic Chemistry published new progress about diethyl chlorophosphite reaction oxygenated functional group. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Recommanded Product: 2,3-Dimethoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Messick, Troy E. published the artcileBiophysical screens identify fragments that bind to the viral DNA-binding proteins EBNA1 and LANA, Product Details of C10H6N2O, the main research area is DNA EBNA1 LANA protein ligand interaction binding fragment NMR; biophys screen surface plasmon resonance saturation transfer difference; Epstein–Barr nuclear antigen 1; Epstein–Barr virus; Kaposi’s sarcoma associated herpesvirus (KSHV); fragment-based lead discovery; latency-associated nuclear antigen; protein–DNA interaction; saturation transfer difference-nuclear magnetic resonance; surface plasmon resonance.

The human gamma-herpesviruses Epstein-Barr virus (EBV) (HHV-4) and Kaposi’s sarcoma-associated herpesvirus (KSHV) (HHV-8) are responsible for a number of diseases, including various types of cancer. Epstein-Barr nuclear antigen 1 (EBNA1) from EBV and latency-associated nuclear antigen (LANA) from KSHV are viral-encoded DNA-binding proteins that are essential for the replication and maintenance of their resp. viral genomes during latent, oncogenic infection. As such, EBNA1 and LANA are attractive targets for the development of small-mol. inhibitors. To this end, we performed a biophys. screen of EBNA1 and LANA using a fragment library by saturation transfer difference (STD)-NMR spectroscopy and surface plasmon resonance (SPR). We identified and validated a number of unique fragment hits that bind to EBNA1 or LANA. We also determined the high-resolution crystal structure of one fragment bound to EBNA1. Results from this screening cascade provide new chem. starting points for the further development of potent inhibitors for this class of viral proteins.

Molecules published new progress about Affinity. 87150-13-8 belongs to class nitriles-buliding-blocks, name is 4-(5-Oxazolyl)benzonitrile, and the molecular formula is C10H6N2O, Product Details of C10H6N2O.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

V., Bhavadhaarani published the artcileCombined treatment of synthetic textile effluent using mixed azo dye by phyto and phycoremediation, Recommanded Product: 2,3-Dimethoxybenzonitrile, the main research area is azo dye textile effluent phytoremediation bioadsorptive wastewater treatment; Phycoremediation; phytoremediation; textile effluent.

Phytoremediation is one of the biol. approaches for remediating textile dyeing effluents. The objective of this study is the use of Pistia stratiotes, an aquatic macrophyte, which was found to degrade the maximum of 83% of mixed azo dye. A phytoreactor was designed and constructed to scale up the process of phytoremediation by P. stratiotes to treat 40mg/l of synthetic textile effluent. Continuous flow phytoreactor fed with 40mg/l (cycle 1) which showed maximum decolorization of 84%, COD removal was about 61%, BOD which was reduced up to 71.9%, and TDS removal was about 72% resp. Further to remove the residual color and toxic effects of the dyes, Phycoremediation was followed for the mixed azo dyes using the microalgae Chlorella vulgaris which showed a maximum decolorization of 99% in the batch study and 74% in the scale-up study where the treated effluent was at the most minimal discharge. Phytotoxicity tests showed 80% of germination in treated effluent, and the plants in untreated wastewater had inhibited growth that indicates only 30% of germination. Such combined biol. treatment techniques were put forward to be the most eco-friendly technol., which is cost-effective and attain zero discharge of the textile effluent.

International Journal of Phytoremediation published new progress about Azo dyes. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Recommanded Product: 2,3-Dimethoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kanaoka, Yuichi published the artcilePolyphosphate ester as a synthetic agent. XII. Convenient synthesis of nitriles by the dehydration of amides with PPE, Application of 2,3-Dimethoxybenzonitrile, the main research area is polyphosphate ester synthesis benzonitrile; benzonitrile polyphosphate ester synthesis; naphthonitrile polyphosphate ester synthesis; furonitrile polyphosphate ester synthesis; nicotinonitrile polyphosphate ester synthesis; cyano cyclohexane polyphosphate ester synthesis; cyclopentane cyano polyphosphate ester synthesis; nitrile benzo polyphosphate ester synthesis.

Nitriles were prepared in improved yields by the dehydration of amides with PPE, prepared from P2O5 and Et2O. Thus, a solution of BzNH2 and PPE in CHCl3 was refluxed 2 hr to give 87% PhCN. m-Nitrobenzonitrile, p-nitrobenzonitrile, o-chlorobenzonitrile, m-hydroxybenzonitrile, p-hydroxybenzonitrile, m-methoxybenzonitrile, p-methoxybenzonitrile, 2,3-dimethoxybenzonitrile, β-naphthonitrile, cyclopentanecarbonitrile, cyclohexanecarbonitrile, phenylacetonitrile, 2-furonitrile, nicotinonitrile, and isonicoinonitrile, were similarly prepared, but 2-furancarboxamide resisted dehydration. The primary amides were prepared by ammonolysis of the corresponding acid chlorides.

Chemical & Pharmaceutical Bulletin published new progress about Nitriles. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Application of 2,3-Dimethoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Procopiou, Panayiotis A. published the artcileSynthesis and Structure-Activity Relationships of Indazole Arylsulfonamides as Allosteric CC-Chemokine Receptor 4 (CCR4) Antagonists, Computed Properties of 221202-34-2, the main research area is indazole arylsulfonamide allosteric CC chemokine receptor 4 antagonist preparation; structure activity relationship solubility clearance human CCR4 antagonist; crystal mol structure indazole thiophenesulfonamide.

A series of indazole arylsulfonamides were synthesized and examined as human CCR4 antagonists. Methoxy- or hydroxyl- containing groups were the more potent indazole C4 substituents. Only small groups were tolerated at C5, C6, or C7, with the C6 analogs being preferred. The most potent N3-substituent was 5-chlorothiophene-2-sulfonamide. N1 meta-substituted benzyl groups possessing an α-amino-3-[(methylamino)acyl]- group were the most potent N1-substituents. Strongly basic amino groups had low oral absorption in vivo. Less basic analogs, such as morpholines, had good oral absorption; however, they also had high clearance. The most potent compound with high absorption in two species was analog I (GSK2239633A), which was selected for further development. Aryl sulfonamide antagonists bind to CCR4 at an intracellular allosteric site denoted site II. X-ray diffraction studies on two indazole sulfonamide fragments suggested the presence of an important intramol. interaction in the active conformation.

Journal of Medicinal Chemistry published new progress about Acidity. 221202-34-2 belongs to class nitriles-buliding-blocks, name is 2,3-Difluoro-6-methoxybenzonitrile, and the molecular formula is C8H5F2NO, Computed Properties of 221202-34-2.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Makosza, Mieczyslaw published the artcileNitroarylamines via the Vicarious Nucleophilic Substitution of Hydrogen: Amination, Alkylamination, and Arylamination of Nitroarenes with Sulfenamides, SDS of cas: 87331-46-2, the main research area is vicarious nucleophilic substitution nitroarylamine preparation; nitroarylamine preparation; arylamine nitro preparation; amination nitroarene sulfenamide.

A new reaction of sulfenamides with electrophilic arenes under basic conditions is described. The σ adducts formed from nitroarenes and the anions of sulfenamides undergo elimination of thiol to produce the corresponding o- and/or p-nitroanilines. This reaction is analogous to the known alkylation and hydroxylation of nitroarenes via the vicarious nucleophilic substitution of hydrogen (VNS). The reaction gives access to a wide range of substituted nitroanilines, nitronaphthylamines, and aminoheterocycles. By means of the reaction with N-alkyl- and N-arylsulfenamides, it is possible to obtain N-alkylnitroanilines and nitrodiarylamines. By varying the structure of sulfenamide and the reaction conditions, particularly the nature and concentration of the base, it is possible to control the orientation of amination.

Journal of Organic Chemistry published new progress about Amination. 87331-46-2 belongs to class nitriles-buliding-blocks, name is 2-Amino-3-nitrobenzonitrile, and the molecular formula is C7H5N3O2, SDS of cas: 87331-46-2.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Groen, Aaron C. published the artcileA novel small-molecule inhibitor reveals a possible role of kinesin-5 in anastral spindle-pole assembly, Formula: C10H8FN, the main research area is FCPT ATPase inhibitor kinesin spindle pole assembly.

The tetrameric plus-end-directed motor, kinesin-5, is essential for bipolar spindle assembly. Small-mol. inhibitors of kinesin-5 have been important tools for investigating its function, and some are currently under evaluation as anti-cancer drugs. Most inhibitors reported to date are ‘non-competitive’ and bind to a specific site on the motor head, trapping the motor in an ADP-bound state in which it has a weak but non-zero affinity for microtubules. Here, we used a novel ATP-competitive inhibitor, FCPT, developed at Merck (USA). We found that it induced tight binding of kinesin-5 onto microtubules in vitro. Using Xenopus egg-extract spindles, we found that FCPT not only blocked poleward microtubule sliding but also selectively induced loss of microtubules at the poles of bipolar spindles (and not asters or monoasters). We also found that the spindle-pole proteins TPX2 and γ-tubulin became redistributed to the spindle equator, suggesting that proper kinesin-5 function is required for pole assembly.

Journal of Cell Science published new progress about Centrosome. 97009-67-1 belongs to class nitriles-buliding-blocks, name is 1-(4-Fluorophenyl)cyclopropanecarbonitrile, and the molecular formula is C10H8FN, Formula: C10H8FN.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Nelson, Derek W. published the artcileStructure-Activity Relationship Studies on a Series of Novel, Substituted 1-Benzyl-5-phenyltetrazole P2X7 Antagonists, Name: 2,3-Dimethoxybenzonitrile, the main research area is enzylphenyltetrazole derivative SAR preparation P2X7 receptor antagonist.

1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X7 receptor. Structure-activity relationship (SAR) studies were conducted around both the benzyl and Ph moieties. In addition, the importance of the regiochem. substitution on the tetrazole was examined Compounds were evaluated for activity to inhibit calcium flux in both human and rat recombinant P2X7 cell lines using fluorometric imaging plate reader technol. Analogs were also assayed for their ability to inhibit IL-1β release and to inhibit P2X7-mediated pore formation in human THP-1 cells. Compound 15d was advanced to efficacy studies in a model of neuropathic pain where significant reversal of mech. allodynia was observed at doses that did not affect motor coordination.

Journal of Medicinal Chemistry published new progress about Allodynia. 5653-62-3 belongs to class nitriles-buliding-blocks, name is 2,3-Dimethoxybenzonitrile, and the molecular formula is C9H9NO2, Name: 2,3-Dimethoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Galdeano, Carles published the artcileStructure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities, Application In Synthesis of 87150-13-8, the main research area is von Hippel Lindau protein ubiquitin ligase hypoxia inducible factor; crystal structure complex thiasole preparation.

E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-mol. ligands has been rewarded with limited success. The von Hippel-Lindau protein (pVHL) is the substrate recognition subunit of the VHL E3 ligase that targets HIF-1α for degradation The authors recently reported inhibitors of the pVHL:HIF-1α interaction, however they exhibited moderate potency. Herein, the authors report the design and optimization, guided by x-ray crystal structures, of a ligand series with nanomolar binding affinities.

Journal of Medicinal Chemistry published new progress about Crystal structure. 87150-13-8 belongs to class nitriles-buliding-blocks, name is 4-(5-Oxazolyl)benzonitrile, and the molecular formula is C10H6N2O, Application In Synthesis of 87150-13-8.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts