Day: February 27, 2023

Ultrasound-sensitive cRGD-modified liposomes as a novel drug delivery system was written by AlSawaftah, Nour M.;Paul, Vinod;Kosaji, Doua;Khabbaz, Leen;Awad, Nahid S.;Husseini, Ghaleb A.. And the article was included in Artificial Cells, Nanomedicine, and Biotechnology in 2022.Electric Literature of C30H26N2O13 This article mentions the following:

Targeted liposomes enable the delivery of encapsulated chemotherapeutics to tumors by targeting specific receptors overexpressed on the surfaces of cancer cells; this helps in reducing the systemic side effects associated with the cytotoxic agents. Upon reaching the targeted site, these liposomes can be triggered to release their payloads using internal or external triggers. In this study, we investigate the use of low-frequency ultrasound as an external modality to trigger the release of a model drug (calcein) from non-targeted and targeted pegylated liposomes modified with cyclic arginine-glycine-aspartate (cRGD). Liposomes were exposed to sonication at 20-kHz using three different power densities (6.2, 9, and 10 mW/cm²). Our results showed that increasing the power d. increased calcein release from the sonicated liposomes. Moreover, cRGD conjugation to the surface of the liposomes rendered cRGD-liposomes more susceptible to ultrasound compared to the non-targeted liposomes. cRGD conjugation was also found to increase cellular uptake of calcein by human colorectal carcinoma (HCT116) cells which were further enhanced following sonicating the cells with low-frequency ultrasound (LFUS). In the experiment, the researchers used many compounds, for example, 2,2′,2”,2”’-(((3′,6′-Dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-2′,7′-diyl)bis(methylene))bis(azanetriyl))tetraacetic acid (cas: 1461-15-0Electric Literature of C30H26N2O13).

2,2′,2”,2”’-(((3′,6′-Dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-2′,7′-diyl)bis(methylene))bis(azanetriyl))tetraacetic acid (cas: 1461-15-0) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Electric Literature of C30H26N2O13

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Dejavu Neural and behavioural effects of the 5-HT₄ receptor agonist, prucalopride, in a hippocampal-dependent memory task was written by de Cates, Angharad N.;Wright, Lucy C.;Martens, Marieke A. G.;Gibson, Daisy;Turkmen, Cagdas;Filippini, Nicola;Cowen, Philip J.;Harmer, Catherine J.;Murphy, Susannah E.. And the article was included in Translational Psychiatry in 2021.Electric Literature of C18H26ClN3O3 This article mentions the following:

Cognitive deficits commonly accompany psychiatric disorders but are often underrecognised, and difficult to treat. The 5-HT4 receptor is a promising potential treatment target for cognitive impairment because in animal studies 5-HT4 receptor agonists enhance hippocampal-dependent memory processes. To date, there has been little work translating these effects to humans. We tested whether short-term administration of the 5-HT4 partial agonist, prucalopride, modified behavioral and neural (fMRI) memory processing in 44 healthy human volunteers using an exptl. medicine model. We found that participants who had received six days of prucalopride treatment were significantly better at recalling previously seen neutral images and distinguishing them from new images. At a neural level, prucalopride bilaterally increased hippocampal activity and activity in the right angular gyrus compared with placebo. Taken together, these findings demonstrate the potential of 5-HT4-receptor activation for cognitive enhancement in humans, and support the potential of this receptor as a treatment target for cognitive impairment. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8Electric Literature of C18H26ClN3O3).

4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Electric Literature of C18H26ClN3O3

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

An improved synthesis of 2-nitrobenzo[b]furans was written by Tromelin, Anne;Demerseman, Pierre;Royer, Rene. And the article was included in Synthesis in 1985.Application of 33094-66-5 This article mentions the following:

Ten nitrobenzofurans I (R = H, MeO, Br, NO₂, MeCO, CO₂Me, cyano; R¹ = H, MeO; R² = H, MeO, Br) were prepared in 2 steps by treating hydroxybenzaldehydes II with BrCH₂NO₂ and K₂CO₃ in Me₂CO to give 48-97% hydroxynitrodihydrobenzofurans III which were dehydrated in refluxing Ac₂O to quant. give I. In the experiment, the researchers used many compounds, for example, 2-Nitrobenzofuran (cas: 33094-66-5Application of 33094-66-5).

2-Nitrobenzofuran (cas: 33094-66-5) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Application of 33094-66-5

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Composition of heterocyclic compounds of oil shale in Cambrian rocks from the east of the Siberian platform was written by Kashirtsev, V. A.;Kovalenko, E. Yu.;Min, R. S.;Sagachenko, T. A.. And the article was included in Khimiya Tverdogo Topliva (Moscow, Russian Federation) in 2009.Related Products of 205-39-0 This article mentions the following:

The mol. composition of the S-, O-, and N-containing heterocyclic aromatic compounds of bitumen separated from the rocks of the Cambrian oil shale formation was studied. Among the sulfur compounds, dibenzothiophene, its alkyl and naphthene derivatives, naphthobenzothiophenes, and their alkyl homologs were identified. Among the oxygen compounds, unbranched dibenzo- and naphthobenzofuran and their C₁-C₄ and C₁-C₂ alkyl homologs, resp., were detected. Acridinones, benzoacridinones, and their alkyl homologs were present among the nitrogen compounds In the experiment, the researchers used many compounds, for example, Naphtho[2,1-b]benzofuran (cas: 205-39-0Related Products of 205-39-0).

Naphtho[2,1-b]benzofuran (cas: 205-39-0) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Related Products of 205-39-0

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Repurposing of the approved small molecule drugs in order to inhibit SARS-CoV-2 S protein and human ACE2 interaction through virtual screening approaches was written by Kalhor, Hourieh;Sadeghi, Solmaz;Abolhasani, Hoda;Kalhor, Reyhaneh;Rahimi, Hamzeh. And the article was included in Journal of Biomolecular Structure and Dynamics in 2022.Computed Properties of C43H51N3O11 This article mentions the following:

Most recently, the new coronavirus (SARS-CoV-2) has been recognized as a pandemic by the World Health Organization (WHO) while this virus shares substantial similarity with SARS-CoV. So far, no definitive vaccine or drug has been developed to cure Covid-19 disease, since many important aspects about Covid-19 such as pathogenesis and proliferation pathways are still unclear. It was proven that human ACE2 is the main receptor for the entry of Covid-19 into lower respiratory tract epithelial cells through interaction with SARS-CoV-2 S protein. Based on this observation, it is expected that the virus infection can be inhibited if protein-protein interaction is prevented. In this study, using structure-based virtual screening of FDA databases, several lead drugs were discovered based on the ACE2-binding pocket of SARS-CoV-2 S protein. Then, binding affinity, binding modes, critical interactions, and pharmaceutical properties of the lead drugs were evaluated. Among the previously approved drugs, Diammonium Glycyrrhizinate, Digitoxin, Ivermectin, Rapamycin, Rifaximin, and Amphotericin B represented the most desirable features, and can be possible candidates for Covid-19 therapies. Furthermore, mol. dynamics (MD) simulation was accomplished for three S protein/drug complexes with the highest binding affinity and best conformation and binding free energies were also computed with the Mol. Mechanics/Poisson-Boltzmann Surface Area (MM/PBSA) method. Results demonstrated the stable binding of these compounds to the S protein; however, in order to confirm the curative effect of these drugs, clin. trials must be done. In the experiment, the researchers used many compounds, for example, (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4Computed Properties of C43H51N3O11).

(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Computed Properties of C43H51N3O11

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Antimicrobial and pesticidal activity of fraxinellone from Dictamnus dasycarpus was written by Yuan, Chunlan;Wang, Xiaoling;Yang, Desuo. And the article was included in Chemical Journal on Internet in 2006.Application of 28808-62-0 This article mentions the following:

By means of solvent partition, preparative TLC, and spectral anal., a main active substance with the biol. activity was fraxinellone contained in D. dasycarpus. Its antifeeding rate and mortality of 72 h at 0.21% (mass percent) against 3rd armyworm (Mythimna separata) were 90.4% and 95.2%, resp. Then antimicrobial activity of fraxinellone had been tested against 7 kinds of bacteria and 10 kinds of plant diseases. The inhibition rate of fraxinellone at 50 ppm reached 100, 99.8, and 99.8% against Escherichia coli, Staphlococcus aureus, and Bacillus megatherium, resp. Its inhibition rate at 100 ppm against Rhizoctonia cerealis van der Hoeven apud. Boerema & Verhoeven was 100% and at 50 ppm against Colletrichurm lagenarium & verhoeven was 72%. In the experiment, the researchers used many compounds, for example, (3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one (cas: 28808-62-0Application of 28808-62-0).

(3R,3aR)-3-(Furan-3-yl)-3a,7-dimethyl-3a,4,5,6-tetrahydroisobenzofuran-1(3H)-one (cas: 28808-62-0) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Application of 28808-62-0

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Optical and structural dynamical behavior of Crystal Violet Lactone – Phenolphthalein binary thermochromic systems was written by Raditoiu, Alina;Raditoiu, Valentin;Nicolae, Cristian Andi;Raduly, Monica Florentina;Amariutei, Viorica;Wagner, Luminita Eugenia. And the article was included in Dyes and Pigments in 2016.Recommanded Product: 1552-42-7 This article mentions the following:

Several binary composites based on Crystal Violet Lactone (CVL) color former and Phenolphthalein (PPht) developing agent dissolved in 1-tetradecanol (TD) were studied in order to determine how different ratios between components influence the thermochromic behavior of the composites. The color dependence on temperature was investigated in direct relationship with structural changes and interactions between components. The stoichiometry of the colored complex was determined from diffuse reflectance data and confirmed by means of steady state fluorescence measurements and temperature modulated differential scanning calorimetry. The color former: developing agent molar ratio equal to 1:2.5 was determined to ensure the reversibility of the process in optimal conditions. The characteristics of the color path and the influence of thermal history during thermochromic transition were analyzed from the variations of CIELAB color parameters during successive heating/cooling cycles. Dynamic colorimetric properties of the thermochromic binary composite containing the components in optimum ratio are described by four characteristic temperatures in the hysteresis. In the experiment, the researchers used many compounds, for example, Crystal violet lactone (cas: 1552-42-7Recommanded Product: 1552-42-7).

Crystal violet lactone (cas: 1552-42-7) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Recommanded Product: 1552-42-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Modification of oligopeptides on aspartic acid or lysine residues by solid-phase synthesis through on-resin side-chain conjugation was written by Ning, Xibo;Liu, Di;Liu, Shimiao;Zhang, Mingjie;Shen, Hongyan. And the article was included in Synlett in 2018.Recommanded Product: 92557-80-7 This article mentions the following:

On-resin side-chain conjugations of various moieties to oligopeptides were performed through an orthogonal protecting protocol using side-chain-protecting groups for aspartic acid or lysine that could be selectively removed on-resin. Various types of modification, such as PEGylation, biotinylation, glycosylation, or fluorophore-labeling of peptides, were realized by using this strategy. The formation of ester, amide, hydrazide, and thiourea bonds was accomplished through the on-resin conjugation. Our work provides an improved and convenient solid-phase synthetic protocol for the modification of oligopeptides on their aspartic acid or lysine residues. This is a universal and practical method that is expected to increase the potential application of peptide-related drugs. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Recommanded Product: 92557-80-7).

2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Recommanded Product: 92557-80-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Acid-base dissociation and tautomerism of two aminofluorescein dyes in solution was written by Mchedlov-Petrossyan, Nikolay O.;Cheipesh, Tatyana A.;Vodolazkaya, Natalya A.. And the article was included in Journal of Molecular Liquids in 2017.Product Details of 3326-34-9 This article mentions the following:

The four-step dissociation of two fluorescein dyes bearing the amino group in 4′- and 5′-positions of the phthalic moiety was studied in water. The constants describing the equilibrium H₄R²⁺⇌H₃R⁺ ⇌ H₂R ⇌ HR- ⇌ R^2- were determined using the spectrophotometric method, at 25 °. In water, four steps of aminofluoresceins dissociation occur within pH range of 0-9. On going to 50 mass % aqueous ethanol, the increase in the pK_a1, pK_a2 and decrease in the pK_a0, pK_a(-1) values take place. The visible absorption spectra, referring to all the ionic (mol.) forms, were singled out. On the whole, the behavior of 4′-aminofluorescein is closer to that of the mother compound The shift of the equilibrium on introducing 50 mass % ethanol into the aqueous solution allowed better understanding the detailed scheme of prototropic equilibrium The tautomeric equilibrium of the mols. shifts toward the colorless lactone. This effect is expressed stronger for the 5′-aminofluorescein. For this dye, even signs of such tautomers of the single-charged anion as anion-lactone and phenolate anion are observed in aqueous ethanol, which are atypical for fluorescein in water-based solvents. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9Product Details of 3326-34-9).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Product Details of 3326-34-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

In vivo pharmacokinetic analyses of placental transfer of three drugs of different physicochemical properties in pregnant rats was written by Mehta, Darshan;Li, Miao;Nakamura, Noriko;Chidambaram, Mani;He, Xiaobo;Bryant, Matthew S.;Patton, Ralph;Davis, Kelly;Fisher, Jeffrey. And the article was included in Reproductive Toxicology in 2022.COA of Formula: C43H51N3O11 This article mentions the following:

Although the use of medication during pregnancy is common, information on exposure to the developing fetus and potential teratogenic effects is often lacking. This study used a rat model to examine the placental transfer of three small-mol. drugs with mol. weights ranging from approx. 300 to 800 Da with different physicochem. properties. Time-mated Sprague Dawley (Hsd:SD) rats aged 11-13 wk were administered either glyburide, rifaximin, or fentanyl at gestational day 15. Maternal blood, placentae, and fetuses were collected at 5 min, 30 min, 1 h, 4 h, 8 h, 24 h, 48 h, and 96 h post-dose. To characterize the rate and extent of placental drug transfer, we calculated several pharmacokinetic parameters such as maximum concentration (Cmax), time to maximum concentration (Tmax), area under the concentration-time curve (AUC), half-life (t1/2), clearance (CL), and volume of distribution (Vd) for plasma, placenta, and fetus tissues. The results indicated showed that fetal exposure was lowest for glyburide, accounting for only 2.2% of maternal plasma exposure as measured by their corresponding AUC ratio, followed by rifaximin (37.9%) and fentanyl (172.4%). The fetus/placenta AUC ratios were found to be 10.7% for glyburide, 11.8% for rifaximin, and 39.1% for fentanyl. These findings suggest that although the placenta acts as a protective shield for the fetus, the extent of protection varies for different drugs and depends on factors such as mol. weight, lipid solubility, transporter-mediated efflux, and binding to maternal and fetal plasma proteins. In the experiment, the researchers used many compounds, for example, (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4COA of Formula: C43H51N3O11).

(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.COA of Formula: C43H51N3O11

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem