Category: naphthyridine

Paudler, William W. published the artcileSkraup synthesis and nuclear magnetic resonance spectra of some methylnaphthyridines, Recommanded Product: 2,7-Dimethyl-1,8-naphthyridine, the publication is Journal of Heterocyclic Chemistry (1967), 4(2), 284-9, database is CAplus.

Some mono- and dimethylnaphthyridines were prepared by the application of the Skraup reaction to various 2- and 4-aminopyridines. The proton N.M.R. spectral data assignments are reported. The chem. shifts of the Me protons are calculated

Journal of Heterocyclic Chemistry published new progress about 14903-78-7. 14903-78-7 belongs to naphthyridine, auxiliary class 6.6_Aromatics,Naphthyridines, name is 2,7-Dimethyl-1,8-naphthyridine, and the molecular formula is C10H10N2, Recommanded Product: 2,7-Dimethyl-1,8-naphthyridine.

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

Kapetanovic, I. M. published the artcileEffects of oral dosing paradigms (gavage versus diet) on pharmacokinetics and pharmacodynamics, Category: naphthyridine, the publication is Chemico-Biological Interactions (2006), 164(1-2), 68-75, database is CAplus and MEDLINE.

In cancer chemopreventive studies, test agents are typically administered via diet, while the preclin. safety studies normally employ oral gavage dosing. Correspondence in pharmacokinetic and pharmacodynamic profiles between the two dosing approaches cannot be assumed a priori. Sulindac, a non-steroidal anti-inflammatory agent with potential chemopreventive activity, was used to assess effects of the two oral dosing paradigms on its pharmacokinetics and pharmacodynamics. Time-dependent concentrations of sulindac and its sulfone metabolite were determined in plasma and potential target organ, mammary gland. Prostaglandin E₂ was used as a pharmacodynamic biomarker and measured in mammary gland. An inverse linear relationship was detected between pharmacodynamic and pharmacokinetic markers, area under the curve for prostaglandin E₂ levels and sulindac sulfone concentrations, resp., in the mammary tissue. Marked differences in pharmacokinetics and pharmacodynamics were observed after administration of sulindac by the two oral dosing paradigms. In general, oral gavage resulted in higher peak and lower trough concentrations of sulindac in plasma and mammary tissue, higher area under concentration-time curve in plasma and mammary tissue, and greater effect on prostaglandin E₂ levels than the corresponding diet dosing. This study illustrates potential pitfalls and limitations in trying to generalize based on data obtained with different oral dosing schemes and their extrapolation to potential efficacy and health risks in humans.

Chemico-Biological Interactions 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, Category: naphthyridine.

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

Fredenhagen, Andreas published the artcileEvaluation of the optimization space for atmospheric pressure photoionization (APPI) in comparison with APCI, COA of Formula: C20H17FO4S, the publication is Journal of Mass Spectrometry (2014), 49(8), 727-736, database is CAplus and MEDLINE.

The usefulness of atm. pressure photoionization (APPI) is difficult to evaluate for unknowns due to the fragmented literature. Specifically, the variation of dopants with a wide set of compounds or the use of APPI in the neg. mode have rarely been explored. Thirty compounds were selected that were not suitable for ESI with a wide variety of functional groups and investigated with atm. pressure chem. ionization (APCI) and APPI in the pos. and neg. ion modes. The influence of the mobile phase (eluents containing acetonitrile or methanol) and – for APPI – four different dopants (acetone, chlorobenzene, toluene, and toluene/anisole) were explored. Stepwise variation of the organic mobile phase allowed to elucidate the ionization mechanism. Atm. pressure photoionization was especially useful for compounds, where the M^鈥? and not the [M + H]⁺ was formed. The dopants chlorobenzene and anisole promoted the formation of mol. ions M^鈥? for about half of the compounds, and its formation was also pos. influenced by the use of mobile phases containing methanol. In the neg. ion mode, APPI offered no advantage toward APCI. Best results were generally achieved with the dopant chlorobenzene, establishing that this dopant is suitable for a wide set of compounds For one quarter of the compounds, significantly better results were achieved with mobile phases containing methanol for both APPI and APCI than those with acetonitrile, but only in the pos. mode. With either of the methods – APPI or APCI – about 10% of the compounds were not detected. Strategies to get results quickly with difficult unknowns will be discussed.

Journal of Mass Spectrometry 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

Jones, Suzanne F. published the artcileA phase I/II study of exisulind in combination with docetaxel/carboplatin in patients with metastatic non-small-cell lung cancer, Synthetic Route of 59973-80-7, the publication is Clinical Lung Cancer (2005), 6(6), 361-366, database is CAplus and MEDLINE.

Exisulind is a sulfone derivative of sulindac that induces apoptosis and demonstrates synergy with docetaxel in lung cancer models. This study evaluated the safety, efficacy, and pharmacokinetic interactions of exisulind and docetaxel/carboplatin in patients with metastatic non-small-cell lung cancer (NSCLC). Fifty-seven patients received 218 cycles of docetaxel (75 mg/m²) and carboplatin (area under the curve, 5.0) in combination with exisulind (125-250 mg orally twice daily). Two complete responses and 9 partial responses were observed among the 47 patients assessable for response (overall response rate, 23%). The median duration of response was 5.9 mo and median survival was 9.4 mo. The 1- and 2-yr survival rates are 35% and 14%, resp. The hematol. toxicities were consistent with those previously reported with docetaxel/carboplatin. The most common nonhematol. toxicities were mild to moderate fatigue, anorexia, nausea, and vomiting. The addition of exisulind to the chemotherapy regimen did not interfere with the metabolism or elimination of docetaxel and vice versa, and docetaxel did not interfere with the pharmacokinetic parameters of exisulind. This trial did not allow direct comparison of patients receiving docetaxel/carboplatin with and without exisulind, but when compared with historical data of docetaxel/carboplatin alone, the addition of exisulind does not appear to enhance antitumor activity, duration of response, or survival. Although preclin. data demonstrate increased apoptosis and prolonged survival for the combination of exisulind and docetaxel, multiple clin. trials do not support further clin. development of this combination regimen in patients with advanced NSCLC.

Clinical Lung Cancer 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, Synthetic Route of 59973-80-7.

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

Mathew, Manna Rachel published the artcilePoly(amino hydroxy naphthalene sulphonic acid) modified glassy carbon electrode; an effective sensing platform for the simultaneous determination of xanthine and hypoxanthine, Application of 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Journal of the Electrochemical Society (2020), 167(4), 047519, database is CAplus.

A rapid, simple and reliable electrochem. sensor for the simultaneous determination of xanthine (XA) and hypoxanthine (HX) based on poly(4-amino-3-hydroxy naphthalene-1-sulfonic acid) [p(AHNSA)] modified glassy carbon electrode (GCE) is reported here. The proposed sensor permit well resolved and well separated peaks for XA and HX in 0.1 M NaOH at comparably lowest potential by square wave voltammetric (SWV) technique. The exptl. parameters required for the electroxidn. of both XA and HX are optimized. For simultaneous determination, the oxidation peak current showed a linear variation in the concentration range 4.0 x 10-4-3.0 x 10-6 M and 2.0 x 10-4-6.0 x 10-6 M with detection limits 7.1 x 10-7 M and 1.5 x 10-6 M for XA for HX, resp. The mechanistic aspects were studied by linear sweep voltammetry (LSV) and the electrode processes were found to be diffusion controlled. The developed sensor was found to have promising application in some real samples like tea and coffee and in physiol. samples with good selectivity and sensitivity.

Journal of the Electrochemical Society 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, Application of 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

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

Thomas, Ambily published the artcileCommunication-Electrooxidation of Dopamine at CoNP-pAHNSA Modified Electrode: A Sensitive Approach to Its Determination, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Journal of the Electrochemical Society (2018), 165(10), B466-B468, database is CAplus.

A voltammetric sensor for the simple and rapid determination of dopamine (DA) has been developed using a glassy carbon electrode modified with cobalt nano/poly (4-amino-3-hyroxy-1-naphthalenesulfonic acid) composite. On square wave voltammetric mode, the modified electrode was found to efficiently catalyze the electrochem. oxidation of DA in 0.1 M PBS (pH 7). Response of DA increased linearly with its concentration in the range 5 脳 10^-5 M to 5 脳 10^-7 M with a limit of detection (LOD) 1.75 脳 10^-8 M. Reliability of the developed sensor in real sample anal. was ascertained successfully by determining DA in artificial blood serum, urine and cerebrospinal fluid (CSF).

Journal of the Electrochemical Society 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 C2H4ClNO, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

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

Kumar, Rajesh published the artcileSynthesis, anti-microbial evaluation, and QSAR studies of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Medicinal Chemistry Research (2012), 21(12), 4301-4310, database is CAplus.

A series of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives was synthesized and tested in vitro for its anti-microbial potential. The results of anti-microbial studies indicated that derivatives I [R¹ = H, R² = R³ = R⁴ = OMe; R¹ = R³ = Cl, R² = R⁴ =H] were found to be most effective ones. The mt-QSAR model for anti-microbial activity revealed the importance of topol. parameter, valence zero-order mol. connectivity index (⁰蠂^v) in describing the anti-microbial activity of synthesized 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives

Medicinal Chemistry Research 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

Dibble, David J. published the artcileAza-Diels-Alder Approach to Diquinolineanthracene and Polydiquinolineanthracene Derivatives, Application of 9,10-Diethynylanthracene, the publication is Organic Letters (2018), 20(3), 502-505, database is CAplus and MEDLINE.

This study describes the synthesis of modular diquinolineanthracene and polydiquinolineanthracene derivatives The reported facile and scalable aza-Diels-Alder-based approach requires mild conditions, proceeds in two steps, uses com. available starting materials, and accommodates varying functionalities. Given the known utility of the acene and quinoline motifs, the synthesized mols. and polymers hold promise for organic electronics applications.

Organic Letters 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 C18H10, Application of 9,10-Diethynylanthracene.

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

Kempe, Hideto published the artcileEnormously extended 蟺-electronic conjugation system of dimeric octaethylporphyrin transmitted with anthracene, Application In Synthesis of 18512-55-5, the publication is Tetrahedron Letters (2014), 55(37), 5164-5169, database is CAplus.

Based on the fact that anthracene (Anth) possesses much higher similarity in electron-releasing ability to porphyrin nucleus than the other polyacenes, the dimeric octaethylporphyrin (OEP) derivatives 4 and 5 (OEP-Anth-OEP) were synthesized and their structure-property relations were examined, as compared with related OEP dimers 1-3. Among them, the derivative 4 showed enormously high electronic communication between two terminal OEP rings, potentially providing a suitable unit of the electronic structure for mol. design of the OEP devices operating with less energy and with higher sensitivity to outside stimuli.

Tetrahedron Letters 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 C18H10, Application In Synthesis of 18512-55-5.

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

Frahm, Silke published the artcileSulindac derivatives inhibit cell growth and induce apoptosis in primary cells from malignant peripheral nerve sheath tumors of NF1-patients, HPLC of Formula: 59973-80-7, the publication is Cancer Cell International (2004), No pp. given, database is CAplus.

Background: Malignant peripheral nerve sheath tumors (MPNSTs) are neoplasms leading to death in most cases. Patients with Neurofibromatosis type 1 have an increased risk of developing this malignancy. The metabolites of the inactive prodrug Sulindac, Sulindac Sulfide and Sulindac Sulfone (Exisulind) are new chemopreventive agents that show promising results in the treatment of different cancer types. In this study we examined the antineoplastic effect of these compounds on primary cells derived from two MPNSTs of Neurofibromatosis type 1 patients. Results: Exisulind and Sulindac Sulfide showed a dramatic time- and dose-dependent growth inhibitory effect with IC50-values of 120 渭M, and 63 渭M, resp. The decrease in viability of the tested cells correlated with induction of apoptosis. Treatment with 500 渭M Exisulind and 125 渭M Sulindac Sulfide for a period of 2 days increased the rate of apoptosis 21-27-fold compared to untreated cells. Reduced expression of RAS-GTP and phosphorylated ERK1/2 was detected in treated MPNST cells. Moreover, elevated levels of phosphorylated SAPK/JNK were found after drug treatment, and low activation of cleaved caspase-3 was seen. Conclusions: Our results suggest that this class of compounds may be of therapeutic benefit for Neurofibromatosis type 1 patients with MPNST.

Cancer Cell International 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, HPLC of Formula: 59973-80-7.

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