Month: November 2022

Biological Activities of Avicennia marina Roots and Leaves Regarding Their Chemical Constituents was written by Al-Mur, Bandar A.. And the article was included in Arabian Journal for Science and Engineering in 2021.Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide The following contents are mentioned in the article:

Abstract: Mangrove plants (focally, Avicennia marina) are resources rich in bioactive substances, and they are considered as promising agents in various biol. activities. Phytochem. analyses of the roots and leaves of Avicennia marina collected from the coast of Jeddah, Saudi Arabia, showed different proportions of various parameters which generally recorded higher values in root samples than those analyzed in leaf samples. The total phenolics in raw plant were 19.7% for roots and 9.5% for the leaf samples. In addition, the total flavonoids of roots and leaves samples in raw plant were rather closed to each other and appeared as 8.8% and 10.9%, resp. In particular, the total phenolics and the total flavonoids in crude extracts of roots exhibited considerable higher values (394.8 and 175.9 mg/L, resp.) than that of leaves (190.8 and 21.7 mg/L, resp.). Both the root and leaves of A. marina showed promising antioxidant activity and thus are very promising agents. Addnl., the results revealed that both crude extracts had effective activities. The most affected bacterial pathogen was Klebsiella pneumoniae which was inhibited by leaves crud extract (24 mm), while Enterococcus faecalis was the lowest inhibited bacterium by the two crudes tested (12 mm). On the other hand, the GC-MS results of methanol extract from the roots and leaves of A. marina showed the presence of several bioactive components, with totally 28 and 26 major compounds, resp., especially fatty acids and their derivatives, which are famous as antioxidant and antibacterial agents. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Safety of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Structural and Optical Properties of Nanocrystalline 3-(2-Benzothiazolyl)-7-(diethylamino) Coumarin (C6) Thin Films for Optoelectronic Application was written by Ebied, Mostafa Saad;Dongol, Mahmoud;Ibrahim, Medhat;Nassary, Mohammed;Elnobi, Sahar;Abuelwafa, Amr Attia. And the article was included in Journal of Electronic Materials in 2022.Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:

In the current work, the structural and optical properties of thermally evaporated 3-(2-Benzothiazolyl)-7-(diethylamino) coumarin [Coumarin 6 (C6)] thin films on a pre-cleaned quartz substrate were studied as a function of the annealing temperature The influence of annealing on the structural, morphol., and mol. structures was investigated by x-ray diffraction (XRD), at. force microscopy (AFM), and Fourier transform IR (FTIR) spectroscopy, resp. The XRD and AFM results confirmed that the as-deposited and annealed films have nanostructural features (30.96-45.34 nm). Also, the increase in roughness of the C6 thin film surface resulted from particle agglomeration and coalescence. Optical constants of C6 thin films were derived from the transmittance T(λ) and reflectance, R(λ) measurements in the spectral range of 200-2500 nm. Anal. of the optical absorption coefficient data indicates that the type of electronic transition in these films is an indirect allowed transition. The estimated optical band gap was decreased from 2.12 eV to 2.01 eV as the annealing temperature was increased. Dispersion and dielec. parameters were determined as functions of the annealing temperature Lastly, nonlinear optical parameters such as the third-order nonlinear susceptibility, χ(3) and nonlinear refractive index, n₍₂₎ were estimated and influenced by annealing temperature The optical properties of C6 thin films were showed that C6 thin films would be used in a wide range of photonic applications Graphical Abstract: [graphic not available: see fulltext]. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Colorful Luminescent Magnetic Supraparticles: Expanding the Applicability, Information Capacity, and Security of Micrometer-Scaled Identification Taggants by Dual-Spectral Encoding was written by Muessig, Stephan;Reichstein, Jakob;Miller, Franziska;Mandel, Karl. And the article was included in Small in 2022.Product Details of 38215-36-0 The following contents are mentioned in the article:

(Sub)micrometer-scaled identification (ID) taggants enable direct identification of arbitrary goods, thereby opening up application fields based on the possibility of tracking, tracing, and anti-counterfeiting. Due to their small dimensions, these taggants can equip in principle even the smallest subcomponents or raw materials with information. To achieve the demanded applicability, the mostly used optically encoded ID taggants must be further improved. Here, micrometer-scaled supraparticles with spectrally encoded luminescent and magnetically encoded signal characteristics are reported. They are produced in a readily customizable bottom-up fabrication procedure that enables precise adjustment of luminescent and magnetic properties on multiple hierarchy levels. The incorporation of commonly used magnetic nanoparticles and fluorescent dyes, resp., into polymer nanocomposite particles, establishes a convenient toolbox of magnetic and luminescent building blocks. The subsequent assembly of selected building blocks in the desired ratios into supraparticles grants for all the flexibility to freely adjust both signal characteristics. The obtained spectrally resolved visible luminescent and invisible magnetic ID signatures are complementary in nature, thus expanding applicability and information security compared to recently reported optical- or magnetic-encoded taggants. Addnl., the introduced ID taggant supraparticles can significantly enhance the coding capacity. Therefore, the introduced supraparticles are considered as next-generation ID taggants. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Product Details of 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Product Details of 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Multifunctional icariin and tanshinone IIA co-delivery liposomes with potential application for Alzheimer’s disease was written by Wang, Jiao;Kong, Liang;Guo, Rui-Bo;He, Si-Yu;Liu, Xin-Ze;Zhang, Lu;Liu, Yang;Yu, Yang;Li, Xue-Tao;Cheng, Lan. And the article was included in Drug Delivery in 2022.Formula: C20H18N2O2S The following contents are mentioned in the article:

The blood-brain barrier (BBB) is a protective barrier for brain safety, but it is also a major obstacle to the delivery of drugs to the cerebral parenchyma such as the hippocampus, hindering the treatment of central nervous system diseases such as Alzheimers disease (AD). In this work, an anti-AD brain-targeted nanodrug delivery system by co-loading icariin (ICA) and tanshinone IIA (TSIIA) into Aniopep-2-modified long-circulating (Ang2-ICA/TSIIA) liposomes was developed. Low-d. lipoprotein receptor-related protein-1 (LRP1) was a receptor overexpressed on the BBB. Angiopep-2, a specific ligand of LRP1, exhibited a high binding efficiency with LRP1. Addnl., ICA and TSIIA, drugs with neuroprotective effects are loaded into the liposomes, so that the liposomes not only have an effective BBB penetration effect, but also have a potential anti-AD effect. The prepared Ang2-ICA/TSIIA liposomes appeared narrow dispersity and good stability with a diameter of 110 nm, and a round morphol. Cell uptake observations, BBB models in vitro, and imaging anal. in vivo showed that Ang2-ICA/TSIIA liposomes not only penetrate the BBB through endocytosis, but also accumulate in N2a cells or brain tissue. The pharmacodynamic anal. in vivo demonstrated that Ang2-ICA/TSIIA liposomes could improve AD-like pathol. features in APP/PS1 mice, including inhibiting neuroinflammation and oxidative stress, reducing apoptosis, protecting neurons, and improving cognitive function. Therefore, Ang2-ICA/TSIIA liposomes are considered a potentially effective therapeutic strategy for AD. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Formula: C20H18N2O2S).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Formula: C20H18N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hirsutanol A inhibits T-acute lymphocytic leukemia Jurkat cell viability through cell cycle arrest and p53-dependent induction of apoptosis was written by Zhong, Fangfang;Yang, You;Ren, Danwei;Long, Sili;Qin, Xiang;Liu, Jing;Zeng, Yan;Lan, Wenjian;Ma, Wenzhe;Liu, Wenjun. And the article was included in Experimental and Therapeutic Medicine in 2021.Quality Control of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide The following contents are mentioned in the article:

Acute lymphocytic leukemia (ALL) is a type of childhood leukemia with the highest incidence; T-acute lymphocytic leukemia (T-ALL) is far more difficult to treat than B-acute lymphocytic leukemia (B-ALL) and has a poor long-term prognosis. Therefore, there is an urgent require- ment to develop effective drugs for the treatment of T-ALL. Hirsutanol A is a natural sesquiterpenoid compound The aim of the present study was to evaluate the in vitro anticancer activity of hirsutanol A against T-acute lymphocytic leukemia Jurkat cells and investigate the mechanism of action. A Cell Counting Kit-8 assay demonstrated that hirsutanol A inhibited the viability of Jurkat cells in a dose- and time-dependent manner. In addition, hirsutanol A induced cell cycle arrest at the G2 phase as determined via flow cytometry. Furthermore, Hoechst staining, Annexin V-FITC/propidium iodide double staining, mitochondrial membrane potential detection using JC-1 and western blot anal. of apoptotic proteins indicated that the inhibitory effect of hirsutanol A on Jurkat cells was associated with the induction of apoptosis. Of note, hirsu- tanol A induced the expression of the tumor suppressor p53, whereas simultaneous treatment with pifithrin-α, an inhibitor of p53, significantly reduced Jurkat cell apoptosis induced by hirsutanol A. In summary, the present study suggested that hirsutanol A inhibited Jurkat cell viability through induction of cell cycle arrest and p53-dependent initiation of apoptosis, thus hirsutanol may serve as a promising compound for the treatment of T-ALL. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Quality Control of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Quality Control of 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Role of fennel oil/ quercetin dual nano-phytopharmaceuticals in hampering liver fibrosis: Comprehensive optimization and in vivo assessment was written by Hafez, Dina Ashraf;Abdelmonsif, Doaa A.;Aly, Rania G.;Samy, Wael Mahmoud;Elkhodairy, Kadria A.;Abo Aasy, Noha Khalifa. And the article was included in Journal of Drug Delivery Science and Technology in 2022.Recommanded Product: 38215-36-0 The following contents are mentioned in the article:

The unmet medical needs related to liver fibrosis and its incurable effects bring to an urgent necessity to find new treatment strategies from which, nutra-pharmaceuticals and nanotechnol. are attracting a considerable interest. The natural flavonoid, quercetin and the essential oil of fennel were proposed for their proven antifibrotic activity. They were successfully loaded in lipid nanocapsules, which were furtherly coated with hyaluronic acid for enhanced CD44active targeting potential. Thorough in vitro optimization produced monodisperse nanocapsules (particle size; 36.78 nm and PDI <0.2). Coating with hyaluronic acid not only sustain quercetin release but also, induce an efficient time dependent accumulation in a highly CD44 expressing cell line, HepG2, opposite to the uncoated nanocapsules. lipid nanocapsules coated with hyaluronic acid and loaded with both quercetin and fennel oil proved a promising synergistic antifibrotic efficiency on rats with CCL4-induced liver fibrosis. In vivo results revealed a significant improvement in liver function tests along with a significant reduction in liver fibrosis markers. Based on the significant downregulation in both liver oxidative stress parameters and hepatic proinflammatory cytokines, mechanism of action can be elucidated to be through antioxidant enzymes activation and inhibition of inflammatory mediators. Concerning toxicity, no reported hematol., hepato-or nephrotoxicity with all formulations, guaranteeing their safety. Hence, tried combination holds a promising treatment to liver fibrosis. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Recommanded Product: 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Recommanded Product: 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Preparation and evaluation of folate-modified albumin baicalin-loaded nanoparticles for the targeted treatment of breast cancer was written by Meng, Fansu;Liu, Fengjie;Lan, Meng;Zou, Tengteng;Li, Lihong;Cai, Tiange;Cai, Yu. And the article was included in Journal of Drug Delivery Science and Technology in 2021.Computed Properties of C20H18N2O2S The following contents are mentioned in the article:

Baicalin (BA) has been shown to be one of the natural compounds with anti-proliferative activity against numerous cancer cell lines, but its application is restricted due to its rapid metabolism and non-targeting to specific tissues. This study exploited folic acid (FA)-conjugated bovine serum albumin (BSA) nanoparticles (NPs) loaded with baicalin (FA-BSANPs/BA) by desolvation crosslinking method to improve its bioavailability and therapeutic efficacy. The optimized FA-BSANPs/BA showed spherical shape and uniform distribution. The average particle size, zeta potential, encapsulation efficiency (EE) and drug loading (DL) of FA-BSANPs/BA were 228.41 ± 2.36 nm, -32.70 ± 1.27 mV, 76.88 ± 0.59% and 7.41 ± 0.23%, resp. X-ray diffraction (XRD) and thermogravimetric (TG) anal. exhibited that the drug was amorphous in the particles. The results of drug release behavior in vitro demonstrated that FA-BSANPs/BA releases BA slowly and continuously. In vitro cytotoxicity test results suggested that the IC₅₀ of FA-BSANPs/BA and BA on MCF-7 cells was 16.7 and 75.96 Μg/mL, resp. The uptake efficiency of FA-BSANPs was significantly higher than that of BSANPs, which leads to a stronger potential for apoptosis. In vivo antitumor studies showed that FA-BSANPs/BA can greatly inhibit tumor growth compared with BA and exhibited the ability to target tumors in MCF-7 xenograft tumor-bearing nude mice. In conclusion, FA-BSANPs/BA improves therapeutic efficacy of BA and reduces side effects by targeting tumors, providing a promising strategy for breast cancer therapy. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Computed Properties of C20H18N2O2S).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Computed Properties of C20H18N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

P53-mediated regulation of mitochondrial dynamics plays a pivotal role in the senescence of various normal cells as well as cancer cells was written by Kim, Young Yeon;Um, Jee-Hyun;Shin, Dong Jin;Jeong, Dae Jin;Hong, Young Bin;Yun, Jeanho. And the article was included in FASEB Journal in 2021.Electric Literature of C16H19BrN2OS The following contents are mentioned in the article:

The tumor suppressor p53 is known as a critical mediator of many cellular processes, including cellular senescence, but its role in mitochondrial dynamics is not fully understood. We have previously shown that p53 regulates mitochondrial dynamics via the PKA-Drp1 pathway to induce cellular senescence. In this study, to further understand the role of p53-dependent regulation of mitochondrial dynamics, the effect of p53 expression on mitochondrial morphol. was examined in various cancer cell lines and normal human cells. We found that p53 induced remarkable mitochondrial elongation and cellular senescence in various cancer cells regardless of their p53 status. p53 also induced mitochondrial elongation in various human primary normal cells, suggesting that p53-mediated mitochondrial elongation is a general phenomenon. Moreover, we found that p53 plays an essential role in mitochondrial elongation in H-Ras-induced cellular senescence and in the replicative senescence of normal human cells. Treatment with the MDM-2 antagonist Nutlin-3a also induced mitochondrial elongation through the PKA-Drp1 pathway in IMR90 normal human cells. Furthermore, the inhibition of PKA activity in late-passage normal cells significantly reduced both mitochondrial elongation and cellular senescence, suggesting that the p53-PKA pathway is essential for maintaining the senescence phenotype in normal cells. Together, these results further confirm the direct regulation of mitochondrial dynamics by p53 and the important role of p53-mediated mitochondrial elongation in cellular senescence. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Electric Literature of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C16H19BrN2OS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Regulated preparation of celastrol-loaded nanoparticle by flash nanoprecipitation was written by Qi, Zhiyao;Qiu, Yuening;Zhong, Zilong;Wang, Junyou;Bian, Wei;Cohen Stuart, Martien A.;Wang, Mingwei. And the article was included in Journal of Drug Delivery Science and Technology in 2022.HPLC of Formula: 38215-36-0 The following contents are mentioned in the article:

Active components in Chinese medicine have shown great effects in treating various illness covering inflammation, obesity, diabetes and cancer. However, most of the active components, e.g. celastrol, suffer from the poor solubility and severe toxicity which limit their practical applications. One of the promising strategies is to load drugs in polymeric nanoparticles (NPs). While so far, most of the drug-loaded NPs were prepared by anti-solvent assembly or precipitation, which is a spontaneous and time-consuming process that provides thermodn. equilibrium NPs with typically low particle yield and drug loading content. Herein, we apply a kinetically controlled method, namely Flash Nanopptn. (FNP), to construct celastrol-loaded NPs. Specifically, solvent streams containing celastrol and biodegradable Dextran-b-PLGA are mixed with anti-solvent streams in a multi-inlet vortex mixer. The fast mixing and co-precipitation provide NPs with well-defined particle radius (80-160 nm, PDI <0.2) and structure, high celastrol loading content (11-63%) and tunable release as well. The regulation is achieved by manipulating the drug concentration and stream velocity (defined as Reynolds number). Moreover, the obtained NPs display efficient inhibition of A549 lung cancer cells, whereas notably reduced cytotoxicity to HL-7702 normal liver cell lines. Our study validates advantages of FNP method on preparing Chinese medicine drug-loaded NPs, and the achieved regulation on particle properties show great potential for boosting the application of Chinese medicine active components. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0HPLC of Formula: 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.HPLC of Formula: 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Exploring the systemic delivery of a poorly water-soluble model drug to the retina using PLGA nanoparticles was written by Zhang, Enqi;Osipova, Nadezhda;Sokolov, Maxim;Maksimenko, Olga;Semyonkin, Aleksey;Wang, MinHui;Grigartzik, Lisa;Gelperina, Svetlana;Sabel, Bernhard A.;Henrich-Noack, Petra. And the article was included in European Journal of Pharmaceutical Sciences in 2021.Category: thiazole The following contents are mentioned in the article:

During the drug development process, many pharmacol. active compounds are discarded because of poor water solubility, but nanoparticle-based formulations are increasingly proposed as a solution for this problem. We therefore studied the distribution of nanoparticulate carriers and the delivery of their poorly water-soluble cargo to a structure of the central nervous system, the retina, under naive and pathol. conditions. The lipophilic fluorescent dye coumarin 6 (Cou6) was encapsulated into poly(lactic-co-glycolic acid) PLGA nanoparticles (NPs). After i.v. administration in rats, we analyzed the distribution of cargo Cou6 and of the NP carrier covalently labeled with Cy5.5 in healthy animals and animals with optic nerve crush (ONC). In vivo real-time retina imaging revealed that Cou6 was rapidly released from PLGA NPs and penetrated the inner blood-retina barrier (BRB) within 15 min and PLGA NPs were gradually eliminated from the retinal blood circulation. Ex vivo microscopy of retinal flat mounts indicated that the Cou6 accumulated predominantly in the extracellular space and to a lesser extent in neurons. While the distribution of Cou6 in healthy animals and post ONC was comparable at early time point post-operation, the elimination of the NPs from the vessels was faster on day 7 post ONC. These results demonstrate the importance of considering different kinetics of nano-carrier and poorly water-soluble cargo, emphasizing the critical role of their parenchymal distribution, i.e. cellular/extracellular, and function of different physiol. and pathol. conditions. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Category: thiazole).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica