Heterocyclic Building Blocks-Naphthyridine

Targeting CK2 in cancer: a valuable strategy or a waste of time? was written by Salvi, Mauro;Borgo, Christian;Pinna, Lorenzo A.;Ruzzene, Maria. And the article was included in Cell Death Discovery in 2021.Computed Properties of C19H12ClN3O2 This article mentions the following:

CK2 is a protein kinase involved in several human diseases (ranging from neurol. and cardiovascular diseases to autoimmune disorders, diabetes, and infections, including COVID-19), but its best-known implications are in cancer, where it is considered a pharmacol. target. Several CK2 inhibitors are available and clin. trials are underway in different cancer types. Recently, the suitability of CK2 as a broad anticancer target has been questioned by the finding that a newly developed compound, named SGC-CK2-1, which is more selective than any other known CK2 inhibitor, is poorly effective in reducing cell growth in different cancer lines, prompting the conclusion that the anticancer efficacy of CX-4945, the commonly used clin.-grade CK2 inhibitor, is to be attributed to its off-target effects. Here we perform a detailed scrutiny of published studies on CK2 targeting and a more in-depth anal. of the available data on SGC-CK2-1 vs. CX-4945 efficacy, providing a different perspective about the actual reliance of cancer cells on CK2. Collectively taken, our arguments would indicate that the pretended dispensability of CK2 in cancer is far from having been proved and warn against premature conclusions, which could discourage ongoing investigations on a potentially valuable drug target. In the experiment, the researchers used many compounds, for example, 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6Computed Properties of C19H12ClN3O2).

5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6) belongs to naphthyridine derivatives. The naphthyridines and their derivatives exhibit various types of biological activity, and the organic chemistry has been frequently reviewed. 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.Computed Properties of C19H12ClN3O2

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

Casein kinase 2 inhibition impairs spontaneous and oxytocin-induced contractions in late pregnant mouse uterus was written by Suhas, K. S.;Parida, Subhashree;Gokul, Chandrasekaran;Srivastava, Vivek;Prakash, E.;Chauhan, Sakshi;Singh, Thakur Uttam;Panigrahi, Manjit;Telang, Avinash G.;Mishra, Santosh K.. And the article was included in Experimental Physiology in 2018.Recommanded Product: 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid This article mentions the following:

The protein kinase casein kinase 2 (CK2) is a ubiquitously expressed serine or threonine kinase known to phosphorylate a number of substrates. The aim of this study was to assess the effect of CK2 inhibition on spontaneous and oxytocin-induced uterine contractions in 19 day pregnant mice. The CK2 inhibitor CX-4945 elicited a concentration-dependent relaxation in late pregnant mouse uterus. CX-4945 and another selective CK2 inhibitor, apigenin, also inhibited the oxytocin-induced contractile response in late pregnant uterine tissue. Apigenin also blunted the prostaglandin F_2a response, but CX-4945 did not. Casein kinase 2 was located in the lipid raft fractions of the cell membrane, and disruption of lipid rafts was found to reverse its effect. The results of the present study suggest that CK2, located in lipid rafts of the cell membrane, is an active regulator of spontaneous and oxytocin-induced uterine contractions in the late pregnant mouse. In the experiment, the researchers used many compounds, for example, 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6Recommanded Product: 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. 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. 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.Recommanded Product: 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid

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

Anti-Growth, Anti-Angiogenic, and Pro-Apoptotic Effects by CX-4945, an Inhibitor of Casein Kinase 2, on HuCCT-1 Human Cholangiocarcinoma Cells via Control of Caspase-9/3, DR-4, STAT-3/STAT-5, Mcl-1, eIF-2α, and HIF-1α was written by Wang, Saini;Yadav, Anil Kumar;Han, Jin-Yi;Ahn, Keun Soo;Jang, Byeong-Churl. And the article was included in International Journal of Molecular Sciences in 2022.Quality Control of 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid This article mentions the following:

Overexpression of casein kinase 2 (CK2) has an oncogenic and pro-survival role in many cancers. CX-4945 (Silmitasertib) is a CK2 inhibitor with anti-cancerous and anti-angiogenic effects. Up to date, the anti-cancer effect and mechanism of CX-4945 on human cholangiocarcinoma (CCA) remain unclear. This study investigated whether CX-4945 inhibits growth and induces apoptosis of HuCCT-1 cells, a human CCA cell line. Of note, treatment with CX-4945 at 20μM markedly reduced survival and induced apoptosis of HuCCT-1 cells, as evidenced by nuclear DNA fragmentation, PARP cleavage, activation of caspase-9/3, and up-regulation of DR-4. Although CX-4945 did not affect the phosphorylation and expression of CK2, it vastly inhibited the phosphorylation of CK2 substrates, supporting the drug’s efficacy in inhibiting CK2 and its downstream pathway. Importantly, knockdown of CK2 that partially suppressed the phosphorylation of CK2 substrates resulted in a significant reduction of HuCCT-1 cell survival. In addition, CX-4945 reduced the phosphorylation and expression of STAT-3 and STAT-5 in HuCCT-1 cells, and pharmacol. inhibition or resp. knockdown of these proteins resulted in significant growth suppression of HuCCT-1 cells. CX-4945 also had abilities to decrease Mcl-1 expression while increasing eIF-2α phosphorylation in HuCCT-1 cells. Furthermore, there was a time-differential neg. regulation of HIF-1α expression by CX-4945 in HuCCT-1 cells, and knockdown of HIF-1α caused a significant reduction of the cell survival. In summary, these results demonstrated that CX-4945 has anti-growth, anti-angiogenic, and pro-apoptotic effects on HuCCT-1 cells, which are mediated through control of CK2, caspase-9/3, DR-4, STAT-3/5, Mcl-1, eIF-2α, and HIF-1α. In the experiment, the researchers used many compounds, for example, 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid (cas: 1009820-21-6Quality Control 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. Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them have a wide range of biological activities. 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.Quality Control of 5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid

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

An Efficient Synthesis of an α_vβ₃ Antagonist was written by Yasuda, Nobuyoshi;Hsiao, Yi;Jensen, Mark S.;Rivera, Nelo R.;Yang, Chunhua;Wells, Kenneth M.;Yau, James;Palucki, Michael;Tan, Lushi;Dormer, Peter G.;Volante, Ralph P.;Hughes, David L.;Reider, Paul J.. And the article was included in Journal of Organic Chemistry in 2004.Name: 7-(Dimethoxymethyl)-1,2,3,4-tetrahydro-1,8-naphthyridine This article mentions the following:

A practical preparation of an α_vβ₃ antagonist, (βS)-6-methoxy-β-[2-oxo-3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1-imidazolidinyl]-3-pyridinepropanoic acid (I), is reported. The antagonist consists of three key components, a tetrahydronaphthyridine moiety, a β-alanine moiety, and a central imidazolidone moiety. The tetrahydronaphthyridine component was prepared using two different methods, both of which relied on variations of the Friedlander reaction to establish the desired regiochem. The β-alanine component was prepared using Davies’ asym. 1,4-addition methodol. as the key stereo-defining step. The central imidazolidone portion was created from these two components using an effective three-step cyclization protocol. Thus, a highly convergent process for the drug candidate was defined. In the experiment, the researchers used many compounds, for example, 7-(Dimethoxymethyl)-1,2,3,4-tetrahydro-1,8-naphthyridine (cas: 204452-91-5Name: 7-(Dimethoxymethyl)-1,2,3,4-tetrahydro-1,8-naphthyridine).

7-(Dimethoxymethyl)-1,2,3,4-tetrahydro-1,8-naphthyridine (cas: 204452-91-5) 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.Name: 7-(Dimethoxymethyl)-1,2,3,4-tetrahydro-1,8-naphthyridine

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

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