Month: November 2022

Anjali published the artcileSynthesis, characterisation, antioxidant and antimicrobial activity of isatin derivatives, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is International Research Journal of Pharmacy (2019), 10(9), 223-230, database is CAplus.

In the present study some novel Schiff bases of isatin I [R = OH, 2-O₂NC₆H₄, 2-Cl-4-O₂NC₆H₃, etc.] were synthesized by condensation of isatin mol. with anilines after performing the mol. docking and ADME prediction. Some new Schiff bases of isatin I were prepared in order to study the antibacterial, antifungal and antioxidant properties. The isatin was synthesized by Sandmeyer method and then its derivatives I were synthesized after obtaining significant results from mol. docking and ADME prediction. The structures of the synthesized compounds I were confirmed by means of IR, ¹H-NMR and elemental anal. Synthesized compounds I were screened for antioxidant activity, among which I [R = 2-Cl-4-O₂NC₆H₃] showed potent activity as antioxidant. Synthesized compounds I showed broad spectrum of antibacterial and antifungal activities.

International Research Journal of Pharmacy published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Shah, Maulin P. published the artcileMicrobial degradation of reactive red by Pseudomonas spp. MPS-2, Synthetic Route of 116-63-2, the publication is Journal of Bioremediation & Biodegradation (2013), 4(6), 1000197/1-1000197/7, database is CAplus.

Azo dyes are a widespread class of poorly biodegradable industrial pollutants. In anaerobic environments, azo bonds are reductively cleaved yielding carcinogenic aromatic amines, many of which are assumed to resist further metabolism by anaerobes bacteria. The latter compounds generally require aerobic conditions for their degradation A reactive group of azo dye called C.I: Reactive Red was found to be degraded using Pseudomonas spp. MPS-79 to α-ketoglutaric acid with transient accumulation of 4-aminobenzenesulfonic acid (sulphanilic acid), 4-amino, 3-hydronaphthalenesulfonic acid and 4-amino, 5-hydronaphthalene 2,7 disulfonic acid as a degradation intermediate in anaerobic facultative batch culture. Color and Total Organic Carbon (TOC) was successfully removed more than 95% and upto 50% resp. There is no significant correlation between pH and oxygen depletion since there is slightly change in pH was observed (pH from 7.21 to 7.25) though the anaerobiosis was found developed throughout the experiment (redox potential from 0.7 to 1.6 mV). The anaerobic metabolism of glucose as co-metabolite also shown to provide the electrons required for the initial reductive cleavage of the azo group. This finding suggest that it is possible to mineralize the azo dye in the environment; thereby, avoiding accumulation of toxic intermediates in the water.

Journal of Bioremediation & Biodegradation published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C14H20BClO2, Synthetic Route of 116-63-2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Woods, Ross M. published the artcileEnantiomeric separation of biaryl atropisomers using cyclofructan based chiral stationary phases, Name: 2,2′-Dimethoxy-1,1′-binaphthalene, the publication is Journal of Chromatography A (2014), 172-181, database is CAplus and MEDLINE.

Normal phase chiral HPLC methods are presented for the enantiomeric separation of 30 biaryl atropisomers including 18 new compounds recently produced via a novel synthetic approach. Three new cyclofructan based chiral stationary phases were evaluated. Separations were achieved for all but six analytes and the LARIHC CF6-P alone provided 15 baseline separations Effects of polar modifiers and temperature effects also were studied. Apparent thermodn. parameters were determined by van’t Hoff plots. Preparative scale methods were developed and employed resulting in the 1st ever isolation of these novel atropisomers in their pure enantiomeric form. Insights into the mechanism of retention and chiral discrimination are presented.

Journal of Chromatography A published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C6H13N3O2, Name: 2,2′-Dimethoxy-1,1′-binaphthalene.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Gergely, Andras published the artcileCorrosion protection of cold-rolled steel with alkyd paint coatings composited with submicron-structure types polypyrrole-modified nano-size alumina and carbon nanotubes, Synthetic Route of 116-63-2, the publication is Materials Science & Engineering, B: Advanced Functional Solid-State Materials (2012), 177(18), 1571-1582, database is CAplus.

This paper is focused on studying corrosion protection of cold-rolled steel with alkyd paint coatings comprising nano-size alumina and either polystyrene-sulfonate (PSS) modified or sulfonated multi-walled carbon nanotube (MWCNT) supported polypyrrole (PPy). Single layer coatings (in thickness of 40 ± 5 μm) comprising PPy deposited alumina and PSS modified MWCNT supported PPy afforded viable protection during the 1 M sodium chloride test. The coatings containing PSS modified and weakly sulfonated MWCNTs (at volume fractions of 9.9 × 10^-4 and 2.5 × 10^-4) with PPy volume fractions of 3.5 × 10^-3 and 2.5 × 10^-3 provided effective corrosion prevention during the 1 M sodium chloride and hydrochloric acid solution tests. While inhibitor particles were characterized by IR spectroscopy, corrosion products formed at the paint-steel interface were studied by XPS. Apart from the electron microscopy observations, rheol. study of three-dimensional structure of the inhibitor particles was performed in dispersions at similar compositions to those used for the paint formulations. Thus, protection mechanism relating to both types of immersion tests is discussed in terms of properties of the inhibitor particles and their microstructure in the coatings.

Materials Science & Engineering, B: Advanced Functional Solid-State Materials published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Synthetic Route of 116-63-2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Park, Gyoosoon published the artcileH-bonding controls the regioselectivities on the acid-catalyzed reaction of fluorenone with phenol derivatives, Product Details of C25H16O, the publication is Bulletin of the Korean Chemical Society (2010), 31(7), 1837-1838, database is CAplus.

The usefulness of the acid-catalyzed reaction of fluorenone with phenol derivatives and the regio-control elements in the process were studied. All ab initio calculations were also carried out. The hydrogen-bonding decisively reveals in the ortho-product. Thus a relative stability of PD-a-OH attributes to intramol. hydrogen-bonding.

Bulletin of the Korean Chemical Society published new progress about 159-62-6. 159-62-6 belongs to naphthyridine, auxiliary class Other Aromatic Heterocyclic,Spiro, name is Spiro[fluorene-9,9′-xanthene], and the molecular formula is C25H16O, Product Details of C25H16O.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Singh, Jatinder published the artcileCoordination-Driven Self-Assembly of Triazole-Based Apoptosis-Inducible Metallomacrocycles, Synthetic Route of 18512-55-5, the publication is ACS Omega (2019), 4(6), 10810-10817, database is CAplus and MEDLINE.

Ru(II)-metallomacrocycles containing 4-pyridyl-1,2,3-triazole moiety were realized by coordination-driven self-assembly. All new compounds were characterized by ESI-MS, elemental anal., ¹H and ¹³C NMR spectroscopies. The mol. structure of metallomacrocycle 8 was established by single-crystal x-ray crystallog. The anticancer activities of metallomacrocycles 5–8 were evaluated by cytotoxicity, cell cycle anal., and related protein expression. Metallomacrocycle 7 showed greatest cytotoxicity in HepG2 human hepatocellular carcinoma cells. Apoptotic HepG2 cells were analyzed when metallomacrocycle 7 was treated. The results suggest that metallomacrocycle 7 induce liver cancer cell death by increasing apoptosis and cell cycle arrest and that it has potential use as an agent for the treatment of human hepatocellular carcinoma.

ACS Omega published new progress about 18512-55-5. 18512-55-5 belongs to naphthyridine, auxiliary class Alkynyl,Anthracene, name is 9,10-Diethynylanthracene, and the molecular formula is C6H16OSi, Synthetic Route of 18512-55-5.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Li, Han published the artcileβ-Catenin signaling: therapeutic strategies in oncology, COA of Formula: C20H17FO4S, the publication is Cancer Biology & Therapy (2002), 1(6), 621-625, database is CAplus and MEDLINE.

A review. Activated Wnt signaling pathways have been found in various human cancers, including those of the colon, liver, endometrium, ovary, prostate, and stomach. As a result, β-catenin is accumulated and becomes transcriptionally active for proliferative genes and oncogenes. Wnt pathway mutations result in biochem. mechanisms yielding inefficient phosphorylation of β-catenin by glycogen synthase kinase 3β (GSK3β) due to APC, β-catenin and/or axin mutations. Therefore, the needs and the opportunity to develop new cancer therapies exist through reversing oncogenic APC/β-catenin/Lef/Tcf signals. Exisulind and analogs are inhibitors of cyclic GMP phosphodiesterases (PDE) that have been shown to activate and induce protein kinase G. The data show PKG regulation of β-catenin in Wnt signaling, accounting, at least in part, for apoptosis induction in treated colon cancer cells carrying either APC or β-catenin mutations. Exisulind and analogs reduce β-catenin via a novel, GSK3β independent processing mechanism. Activated PKG directly phosphorylate β-catenin at its C-terminal domain and causes proteasome dependent degradation of the protein. Since this pathway is independent of APC and GSK3β, exisulind and analogs provide a superior approach to circumvent the mol. defects of Wnt signaling pathway and to treat cancers with such defects.

Cancer Biology & Therapy published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, COA of Formula: C20H17FO4S.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Yoon, Jung-Taek published the artcileCP248, a derivative of exisulind, causes growth inhibition, mitotic arrest, and abnormalities in microtubule polymerization in glioma cells, Category: naphthyridine, the publication is Molecular Cancer Therapeutics (2002), 1(6), 393-404, database is CAplus and MEDLINE.

Exisulind (sulindac sulfone) and two potent derivatives, CP248 and CP461, have been shown previously to cause growth inhibition and apoptosis in several types of human carcinoma cell lines. These and related compounds have not been previously studied with respect to glioma cell lines. In the present study, we found that these three compounds caused marked growth inhibition in four rat glioma and eight human glioma cell lines, with IC₅₀ values of 150, 1, and 0.075 μM, resp. When studied at these concentrations exisulind and CP461 had no significant effect on the cell cycle profile of glioma cells, but CP248 caused marked arrest in mitosis. Detailed studies of CP248 in the 9L rat gliosarcoma cell line indicated that treatment with 0.075 μM CP248 caused abnormalities in the spindle apparatus and activation of the spindle assembly check point. In interphase glioma cells, CP248 stabilized microtubules (MTs) at low concentrations (0.075 μM) and depolymerized MTs at higher concentrations (0.2-0.4 μM). In NIH 3T3 fibroblasts, 0.1 μM CP248 caused extensive MT depolymerization CP248 also caused MT depolymerization when added to assembled MTs in vitro, which indicated that it can directly affect MTs, perhaps because it shares certain structural similarities with Colcemid. In glioma cells, the effects of CP248 on MTs were independent of the previously reported effects of this compound on activation of protein kinase G. Therefore, CP248 is a novel MT-active agent that may be useful in the treatment of glioblastoma, and possibly other types of cancer, because of its dual effects on protein kinase G and MTs.

Molecular Cancer Therapeutics published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C9H8BNO2, Category: naphthyridine.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Lee, Jin Kyung published the artcileSulindac and its metabolites inhibit multiple transport proteins in rat and human hepatocytes, Recommanded Product: Sulindac sulfone, the publication is Journal of Pharmacology and Experimental Therapeutics (2010), 334(2), 410-418, database is CAplus and MEDLINE.

Sulindac is a commonly used nonsteroidal anti-inflammatory drug. This study tested the hypothesis that sulindac-mediated drug-drug interactions and/or hepatotoxicity may be caused, in part, by inhibition of proteins responsible for the hepatic transport of drugs and/or bile acids by sulindac and/or sulindac metabolites [sulindac sulfone (S-sulfone) and sulindac sulfide (S-sulfide)]. The uptake and excretion of model substrates, [³H]taurocholate (TC), [³H]estradiol 17-β-glucuronide (E217G), and nitrofurantoin (NF), were investigated in rat and human suspended and sandwich-cultured hepatocytes (SCH). In suspended rat hepatocytes, S-sulfone and S-sulfide inhibited Na⁺-dependent TC initial uptake (IC₅₀ of 24.9 ± 6.4 and 12.5 ± 1.8 μM, resp.) and Na⁺-independent E217G initial uptake (IC₅₀ of 12.1 ± 1.6 and 6.3 ± 0.3 μM, resp.). In rat SCH, sulindac metabolites (100 μM) decreased the in vitro biliary clearance (Cl_biliary) of TC, E217G, and NF by 38 to 83%, 81 to 97%, and 33 to 57%, resp.; S-sulfone and S-sulfide also decreased the TC and NF biliary excretion index by 39 to 55%. In suspended human hepatocytes, S-sulfone and S-sulfide inhibited Na⁺-dependent TC initial uptake (IC₅₀ of 42.2 and 3.1 μM, resp.); S-sulfide also inhibited the TC Cl_biliary in human SCH. Sulindac/metabolites markedly inhibited hepatic uptake and biliary excretion of E217G by 51 to 100% in human SCH. In conclusion, sulindac and metabolites are potent inhibitors of the uptake and biliary clearance of bile acids in rat and human hepatocytes and also inhibit substrates of rat breast cancer resistance protein, rat and human organic anion-transporting polypeptides, and human multidrug resistance-associated protein 2. Inhibition of multiple hepatic transport proteins by sulindac/metabolites may play an important role in clin. significant sulindac-mediated drug-drug interactions and/or liver injury.

Journal of Pharmacology and Experimental Therapeutics published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, Recommanded Product: Sulindac sulfone.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Wood, Natasha C. L. published the artcileMediated electron transfer from lithium investigated voltammetrically in tetrahydrofuran: why are some mediators more effective reducing reagents than others?, SDS of cas: 2960-93-2, the publication is Journal of Physical Organic Chemistry (2007), 20(10), 732-742, database is CAplus.

A study of a range of aromatic mols. was studied electrochem. to determine what makes an effective reducing mediator. With the aim of developing a better understanding of electron transfers (ETs) mediated from Li in functional group reduction, single ET reactions are reported. Typical reaction conditions involved the use of aromatic mediators such as naphthalene, anthracene, 4,4′-di-tert-butyl-1,1′-biphenyl (DBB) with Li metal in THF at -78°. The results of these experiments showed that some mediators were more effective reducing reagents than others. Cryoelectrochem. procedures are used to mimic the conditions of the SET (single electron transfer) reactions to study the exact nature and role of the mediator formed upon ET. Electrogenerated and stabilized radical anions of anthracene at -78° mediate the reduction of organic substrates, whereas the more reactive dianion is quickly protonated and therefore unable to act as an ET reagent; direct electrochem. reduction of the sulfide, Ph 3-phenylpropyl sulfide (RSPh) gives the thiol, thiophenol, and propylbenzene whereas mediated reduction gives the dimer, di-Ph disulfide and Pr benzene. The possibility to selectively reduce a substrate with either a single electron or with 2 electrons is possible by using either the radical anion (mediated) or via the direct electroreduction DBB and naphthalene (both single electron accepting species only) are the most effective reducing reagents. Anthracene and other 2-electron accepting species only showed effective reducing ability when a stoichiometric amount of Li was used therefore preventing the over-reduction to the dianion.

Journal of Physical Organic Chemistry published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C18H21BO4, SDS of cas: 2960-93-2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem