Month: February 2023

The Global Phosphorylation Landscape of SARS-CoV-2 Infection was written by Bouhaddou, Mehdi;Memon, Danish;Meyer, Bjoern;White, Kris M.;Rezelj, Veronica V.;Correa Marrero, Miguel;Polacco, Benjamin J.;Melnyk, James E.;Ulferts, Svenja;Kaake, Robyn M.;Batra, Jyoti;Richards, Alicia L.;Stevenson, Erica;Gordon, David E.;Rojc, Ajda;Obernier, Kirsten;Fabius, Jacqueline M.;Soucheray, Margaret;Miorin, Lisa;Moreno, Elena;Koh, Cassandra;Tran, Quang Dinh;Hardy, Alexandra;Robinot, Remy;Vallet, Thomas;Nilsson-Payant, Benjamin E.;Hernandez-Armenta, Claudia;Dunham, Alistair;Weigang, Sebastian;Knerr, Julian;Modak, Maya;Quintero, Diego;Zhou, Yuan;Dugourd, Aurelien;Valdeolivas, Alberto;Patil, Trupti;Li, Qiongyu;Huttenhain, Ruth;Cakir, Merve;Muralidharan, Monita;Kim, Minkyu;Jang, Gwendolyn;Tutuncuoglu, Beril;Hiatt, Joseph;Guo, Jeffrey Z.;Xu, Jiewei;Bouhaddou, Sophia;Mathy, Christopher J. P.;Gaulton, Anna;Manners, Emma J.;Felix, Eloy;Shi, Ying;Goff, Marisa;Lim, Jean K.;McBride, Timothy;O’Neal, Michael C.;Cai, Yiming;Chang, Jason C. J.;Broadhurst, David J.;Klippsten, Saker;De wit, Emmie;Leach, Andrew R.;Kortemme, Tanja;Shoichet, Brian;Ott, Melanie;Saez-Rodriguez, Julio;tenOever, Benjamin R.;Mullins, R. Dyche;Fischer, Elizabeth R.;Kochs, Georg;Grosse, Robert;Garcia-Sastre, Adolfo;Vignuzzi, Marco;Johnson, Jeffery R.;Shokat, Kevan M.;Swaney, Danielle L.;Beltrao, Pedro;Krogan, Nevan J.. And the article was included in Cell (Cambridge, MA, United States) in 2020.Synthetic Route of C19H12ClN3O2 This article mentions the following:

The causative agent of the coronavirus disease 2019 (COVID-19) pandemic, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions and killed hundreds of thousands of people worldwide, highlighting an urgent need to develop antiviral therapies. Here, we present a quant. mass spectrometry-based phosphoproteomics survey of SARS-CoV-2 infection in Vero E6 cells, revealing dramatic rewiring of phosphorylation on host and viral proteins. SARS-CoV-2 infection promoted casein kinase II (CK2) and p38 MAPK activation, production of diverse cytokines, and shutdown of mitotic kinases, resulting in cell cycle arrest. Infection also stimulated a marked induction of CK2-containing filopodial protrusions possessing budding viral particles. Eighty-seven drugs and compounds were identified by mapping global phosphorylation profiles to dysregulated kinases and pathways. We found pharmacol. inhibition of the p38, CK2, CDK, AXL, and PIKFYVE kinases to possess antiviral efficacy, representing potential COVID-19 therapies. In the experiment, the researchers used many compounds, for example, 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6Synthetic Route of C19H12ClN3O2).

5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6) belongs to naphthyridine derivatives. The naphthyridines have 10 delocalized π-electrons located in five molecular orbitals, each of which is distorted by the presence of the nitrogen atoms causing an electron drift in that direction. Transition metal complexes of 1,5-naphthyridine (1,5-napy) seems to form one-dimensional coordination polymers with the ligand acting as bidentate in a “stepped” bridging fashion.Synthetic Route of C19H12ClN3O2

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zero-order release and bioavailability enhancement of poorly water soluble Vinpocetine from self-nanoemulsifying osmotic pump tablet was written by El-Zahaby, Sally A.;Abou Ghaly, Mohamed H. H.;Abdelbary, Ghada A.;El-Gazayerly, Omaima N.. And the article was included in Pharmaceutical Development and Technology in 2018.SDS of cas: 42971-09-5 This article mentions the following:

Solid self-nanoemulsifying (S-SNEDDS) asym. coated osmotic tablets of the poorly water-soluble drug Vinpocetine (VNP) were designed. The aim was to control the release of VNP by the osmotic technol. taking advantage of the solubility and bioavailability-enhancing capacity of S-SNEDDS. Liquid SNEDDS loaded with 2.5 mg VNP composed of Maisine 35-1, Transcutol HP, and Cremophor EL was adsorbed on the solid carrier Aeroperl. S-SNEDDS was mixed with the osmotic tablet excipients (sodium chloride, Avicel, HPMC-K4M, PVP-K30, and Lubripharm), then directly compressed to form the core tablet. The tablets were dip coated and mech. drilled. A 32*21 full factorial design was adopted. The independent variables were: type of coating material (X1), concentration of coating solution (X2), and number of drills (X3). The dependent variables included % release at 2 h (Y1), at 4 h (Y2), and at 8 h (Y3). The in vivo performance of the optimum formula was assessed in rabbits. Zero-order VNP release was obtained by the single drilled 1.5% Opadry CA coated osmotic tablets and twofold increase in VNP bioavailability was achieved. The combination of SNEDDS and osmotic pump tablet system was successful in enhancing the solubility and absorption of VNP as well as controlling its release. In the experiment, the researchers used many compounds, for example, (41S,13aS)-Ethyl 13a-ethyl-2,3,41,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylate (cas: 42971-09-5SDS of cas: 42971-09-5).

(41S,13aS)-Ethyl 13a-ethyl-2,3,41,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylate (cas: 42971-09-5) belongs to naphthyridine derivatives. The naphthyridines and their derivatives exhibit various types of biological activity, and the organic chemistry has been frequently reviewed. Imidazonaphthyridines have been prepared through a ‘one-pot’ three-component ‘domino’ reaction between the keto-ester, acrolein, and ethylenediamine in presence of 4 Å molecular sieves. The corresponding thiazolonaphthyridine is obtained from a similar reaction using 2-aminoethanethiol and Dowex basic anion-exchange resin.SDS of cas: 42971-09-5

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Proteomic investigation reveals dominant alterations of neutrophil degranulation and mRNA translation pathways in patients with COVID-19 was written by Bankar, Renuka;Suvarna, Kruthi;Ghantasala, Saicharan;Banerjee, Arghya;Biswas, Deeptarup;Choudhury, Manisha;Palanivel, Viswanthram;Salkar, Akanksha;Verma, Ayushi;Singh, Avinash;Mukherjee, Amrita;Pai, Medha Gayathri J.;Roy, Jyotirmoy;Srivastava, Alisha;Badaya, Apoorva;Agrawal, Sachee;Shrivastav, Om;Shastri, Jayanthi;Srivastava, Sanjeeva. And the article was included in iScience in 2021.Application In Synthesis of 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid This article mentions the following:

The altered mol. proteins and pathways in response to COVID-19 infection are still unclear. Here, we performed a comprehensive proteomics-based investigation of nasopharyngeal swab samples from patients with COVID-19 to study the host response by employing simple extraction strategies. Few of the host proteins such as interleukin-6, L-lactate dehydrogenase, C-reactive protein, Ferritin, and aspartate aminotransferase were found to be upregulated only in COVID-19-pos. patients using targeted multiple reaction monitoring studies. The most important pathways identified by enrichment anal. were neutrophil degranulation, interleukin-12 signaling pathways, and mRNA translation of proteins thus providing the detailed investigation of host response in COVID-19 infection. Thus, we conclude that mass spectrometry-detected host proteins have a potential for disease severity progression; however, suitable validation strategies should be deployed for the clin. translation. Furthermore, the in silico docking of potential drugs with host proteins involved in the interleukin-12 signaling pathway might aid in COVID-19 therapeutic interventions. In the experiment, the researchers used many compounds, for example, 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6Application In Synthesis of 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid).

5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6) belongs to naphthyridine derivatives. Six naphthyridine isomers exist, based on the positions of the nitrogen atoms; they can be in the 1,5, 1,6, 1,7, 1,8, 2,6, or 2,7 positions. Transition metal complexes of 1,5-naphthyridine (1,5-napy) seems to form one-dimensional coordination polymers with the ligand acting as bidentate in a “stepped” bridging fashion.Application In Synthesis of 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: Possible confounding effects on in vivo and in vitro studies was written by McElhinny, Charles J.;Lewin, Anita H.;Mascarella, S. Wayne;Runyon, Scott;Brieaddy, Lawrence;Carroll, F. Ivy. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Recommanded Product: 792173-99-0 This article mentions the following:

SB-334867 has been an important ligand for the study of the orexin 1 (OX1) receptor due to its high OX1/OX2 selectivity and bioavailability. This ligand however, contains a 2-methylbenzoxazole ring system which is known to undergo hydrolysis, particularly under acidic or basic conditions. The possibility that SB-334867 would be susceptible to significant hydrolysis was evaluated in various formulations and in the solid state. SB-334867 was found to be unstable under conditions commonly employed to prepare stock solutions for in vitro and in vivo studies. In addition, and most alarmingly, the hydrochloride salt of SB-334867 was found to quant. decompose to an OX1-inactive product even in the solid state. These findings combine to suggest that studies using SB-334867 (and any other 2-methylbenzoxazole-containing compound) should be performed with great care to avoid the confounding effects of the rapid hydrolytic decomposition of this susceptible structure. In the experiment, the researchers used many compounds, for example, 1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea (cas: 792173-99-0Recommanded Product: 792173-99-0).

1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea (cas: 792173-99-0) belongs to naphthyridine derivatives. Six naphthyridine isomers exist, based on the positions of the nitrogen atoms; they can be in the 1,5, 1,6, 1,7, 1,8, 2,6, or 2,7 positions. Transition metal complexes of 1,5-naphthyridine (1,5-napy) seems to form one-dimensional coordination polymers with the ligand acting as bidentate in a “stepped” bridging fashion.Recommanded Product: 792173-99-0

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Reactions of 1,5- and 1,8-naphthyridine 1-oxides with phosphorus oxide tribromide was written by Czuba, Wladyslaw;Grzegozek, Maria. And the article was included in Universitatis Iagellonicae Acta Chimica in 1991.Electric Literature of C8H4Br2N2 This article mentions the following:

Reactions of 1,5- and 1,8-naphthyridine 1-oxides and 1,5-naphthyridine 1,5-dioxide with POBr₃ were studied. The characteristic feature of these reactions was high contribution of unsubstituted naphthyridines and 3-bromo derivatives, apart from 2- and 4-bromonaphthyridines, in the reaction products. In the experiment, the researchers used many compounds, for example, 3,7-Dibromo-1,5-naphthyridine (cas: 17965-72-9Electric Literature of C8H4Br2N2).

3,7-Dibromo-1,5-naphthyridine (cas: 17965-72-9) belongs to naphthyridine derivatives. Functionalized naphthyridines and their benzo/heterofused analogs are present in numerous marine products and reported to possess wide-ranging activities such as antiproliferative, antiaggressive, and HIV-1 integrase inhibition in addition to their use as anti-HCV agents. 1,6-Naphthyridine and some of its derivatives have been reported to have medicinal, electronic, and catalytic properties. But none of these investigations has yet resulted in any practical applications. Very few metal complexes of naphthyridines other than 1,8-naphthyridine have been described.Electric Literature of C8H4Br2N2

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Statistical optimization of nanostructured gels for enhancement of vinpocetine transnasal and transdermal permeation was written by El-Dahmy, Rania Moataz;Elshafeey, Ahmed Hassen;Abd El Gawad, Nabaweya Abdelaziz;El-Gazayerly, Omaima Naim;Elsayed, Ibrahim. And the article was included in Journal of Drug Delivery Science and Technology in 2021.Application of 42971-09-5 This article mentions the following:

Pluronic-based nanostructured gels were developed and optimized to increase the permeability of vinpocetine through the skin and the mucous layer of the nasal cavity. A modified thin-film hydration technique was utilized to prepare the nanostructured gel formulas containing different concentrations of Pluronic F127, Pluronic F68 and oleic acid. The formed nanodispersions were tested for their pH, particle size, zeta potential, polydispersity index, entrapment efficiency and gelation temperature Box-Behnken statistical design was used to choose the optimized nasal and transdermal nanostructured gel formulas utilizing Design-Expert software. The nasal optimized formula consisted of 2.4% oleic acid, 23.46% total surfactants and 27.13% Pluronic F68, had a gelation temperature of 35°C which could be suitable to form in situ gel upon application into the nasal cavity. On the other hand, the transdermal optimized formula, composed of 1.77% oleic acid, 22.46% total surfactants and 11.54% Pluronic F68, formed gel at room temperature that could be suitable to be applied onto the skin. The optimized gel formulas were investigated for their in vitro drug release, rheol., morphol., histopathol. and ex vivo permeation. The extent of drug permeated from the optimized formula through both nasal and skin membranes was significantly increased by 3.39 and 4.7 folds when compared to the drug suspension. Finally, the obtained findings ensured the creditable impact of the nanostructured gels as promising nanocarriers for enhancing transmucosal and transdermal vinpocetine permeation. In the experiment, the researchers used many compounds, for example, (41S,13aS)-Ethyl 13a-ethyl-2,3,41,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylate (cas: 42971-09-5Application of 42971-09-5).

(41S,13aS)-Ethyl 13a-ethyl-2,3,41,5,6,13a-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylate (cas: 42971-09-5) belongs to naphthyridine derivatives. The naphthyridines and their derivatives exhibit various types of biological activity, and the organic chemistry has been frequently reviewed. Imidazonaphthyridines have been prepared through a ‘one-pot’ three-component ‘domino’ reaction between the keto-ester, acrolein, and ethylenediamine in presence of 4 Å molecular sieves.Application of 42971-09-5

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem