Tag: 200-300

Evaluation of the Influence of Compound Structure on Stacked-Dimer Formation in the DNA Minor Groove was written by Wang, Lei;Carrasco, Carolina;Kumar, Arvind;Stephens, Chad E.;Bailly, Christian;Boykin, David W.;Wilson, W. David. And the article was included in Biochemistry in 2001.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone This article mentions the following:

The Human Genome Project as well as sequencing of the genomes of other organisms offers a wealth of DNA targets for both therapeutic and diagnostic applications, and it is important to develop addnl. DNA binding motifs to fully exploit the potential of this new information. We have recently found that an aromatic dication, DB293, with an amidine-phenyl-furan-benzimidazole-amidine structure can recognize specific sequences of DNA by binding in the minor groove as a dimer. The dimer binding is strong, highly cooperative and, in contrast to many closely related heterocyclic dications, has both GC and AT base pairs in the minor groove binding site. The aromatic heterocycle stacked dimer is quite different in structure from the polyamide-lexitropsin type compounds, and it is a dication while all lexitropsin dimers are monocations. The heterocyclic dimer represents only the second small mol. class that can recognize mixed sequences of DNA. To test the structural limits on the new type of complex, it is important to probe the influence of compound charge, chem. groups, and structural features. The effects of these compound mol. variations on DNA complex formation with several DNA sequences were evaluated by DNase I footprinting, CD and UV spectroscopy, thermal melting, and quant. anal. with surface plasmon resonance biosensor methods. Conversion of the amidines to guanidinium groups does permit the cooperative dimer to form but removal of one amidine or addition of an alkyl group to the amidine strongly inhibited dimer formation. Changing the Ph of DB293 to a benzimidazole or the benzimidazole to a Ph or benzofuran also inhibited dimer formation. The results show that formation of the minor groove stacked-dimer complex is very sensitive to compound structure. The discovery of the aromatic dimer mode offers new opportunities to enhance the specificity and expand the range of applications of the compounds that target DNA. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) 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: 1-(5-Bromobenzofuran-2-yl)ethanone

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Enantioselective Rh-catalyzed transfer hydrogenation of α-sulfonyloxy heteroaryl ketones; asymmetric synthesis of (S)-bufuralol was written by Kwak, Se Hun;Lee, Do-Min;Lee, Kee-In. And the article was included in Tetrahedron: Asymmetry in 2009.Application of 38220-75-6 This article mentions the following:

Asym. transfer hydrogenation of α-sulfonyloxy heteroaryl ketones mediated by Cp_*RhCl[(S,S)-TsDPEN] using an azeotropic mixture of formic acid/triethylamine afforded the corresponding 2-monosulfonated diols in excellent yield with high enantioselectivity. This led to the asym. synthesis of (S)-bufuralol. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Application of 38220-75-6).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) 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 antiviral, antimicrobial, antitumor, anti-inflammatory.Application of 38220-75-6

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Protective actions of bioactive flavonoids chrysin and luteolin on the glyoxal induced formation of advanced glycation end products and aggregation of human serum albumin: In vitro and molecular docking analysis was written by Sarmah, Sharat;Das, Sourav;Roy, Atanu Singha. And the article was included in International Journal of Biological Macromolecules in 2020.Synthetic Route of C17H10O4 This article mentions the following:

The post-translational modification of proteins by nonenzymic glycation (NEG) and the accumulation of AGEs are the two underlying factors associated with the long-term pathogenesis in diabetes. Glyoxal (GO) is a reactive intermediate which has the ability to modify proteins and generate AGEs at a faster rate. Human serum albumin (HSA) being the most abundant serum protein has a higher chance to be modified by NEG. The key objective of the present study is to investigate the potency of chrysin and luteolin as antiglycating and antifibrillating agents in the GO-mediated glycation and fibril formation of HSA. AGEs formation were confirmed from the absorption and fluorescence spectral measurements. Both the flavonoids were able to quench the AGEs fluorescence intensity in vitro indicating the antiglycating nature of the mols. The formation of fibrils in the GO-modified HSA was confirmed by the Thioflavin T (ThT) fluorescence assay and the flavonoids were found to exihibit the antifibrillation properties in vitro. Docking results suggested that both the flavonoids interact with various amino acid residues of subdomain IIA including glycation prone lysines and arginines via non-covalent forces and further stabilized the structure of HSA, which further explains their mechanisms of action as antiglycating and antifibrillating agents. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Synthetic Route of C17H10O4).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Synthetic Route of C17H10O4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Structure-in vitro activity relationships of pentamidine analogs and dication-substituted bis-benzimidazoles as new antifungal agents was written by Del Poeta, Maurizio;Schell, Wiley A.;Dykstra, Christine C.;Jones, Susan;Tidwell, Richard R.;Czarny, Agnieszka;Bajic, Miroslav;Bajic, Marina;Kumar, Arvind;Boykin, David;Perfect, John R.. And the article was included in Antimicrobial Agents and Chemotherapy in 1998.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone This article mentions the following:

Twenty analogs of pentamidine (including I), 7 primary metabolites of pentamidine, and 30 dicationic substituted bisbenzimidazoles were screened for their inhibitory and fungicidal activities against Candida albicans and Cryptococcus neoformans. A majority of the compounds had MICs at which 80% of the strains were inhibited (MIC₈₀s) comparable to those of amphotericin B and fluconazole. Unlike fluconazole, many of these compounds, such as II and III, were found to have potent fungicidal activity. The most potent compound against C. albicans had an MIC₈₀ of ≤0.09 μg/mL, and the most potent compound against C. neoformans had an MIC₈₀ of 0.19 μg/mL. Selected compounds, such as IV, were also found to be active against Aspergillus fumigatus, Fusarium solani, Candida species other than C. albicans, and fluconazole-resistant strains of C. albicans and C. neoformans. It is clear from the data presented here that further studies on the structure-activity relationships, mechanisms of action and toxicities, and in vivo efficacies of these compounds are warranted to determine their clin. potential. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) 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. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Recommanded Product: 1-(5-Bromobenzofuran-2-yl)ethanone

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Preparation of benzo[b]furans having five-membered heterocycles at the 2-position and 2-(4-alkylcarbamoylbuta-1,3-dienyl)benzo[b]furans, and their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity was written by Akai, Yukiko;Tabuchi, Yukako;Ando, Kumiko;Ito, Azusa;Sakata, Yoko;Kawasaki, Ikuo;Ohishi, Takahiro;Yamashita, Masayuki;Ohta, Shunsaku;Nishide, Kiyoharu;Ohishi, Yoshitaka. And the article was included in Chemical & Pharmaceutical Bulletin in 2012.Formula: C10H7BrO2 This article mentions the following:

A series of benzo[b]furan derivatives having a 5-membered heterocyclic substituent at the 2-position were prepared from 2-(1-chloro-2-formylvinyl)benzo[b]furans and 2-[4-(alkylcarbamoyl)buta-1,3-dienyl]benzo[b]furans. The newly prepared 2-heterocyclic benzo[b]furans were evaluated for their cysteinyl leukotriene receptor (cysLT1, cysLT2) inhibitory activity. Several compounds showed moderate inhibition of Ca mobilization in HEK 293T-cysLT2 or CHO-cysLT1 cells. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Formula: C10H7BrO2).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Formula: C10H7BrO2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Biocompatible antimicrobial electrospun nanofibers functionalized with ε-poly-L-lysine was written by Amariei, Georgiana;Kokol, Vanja;Vivod, Vera;Boltes, Karina;Leton, Pedro;Rosal, Roberto. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2018.Category: benzofurans This article mentions the following:

The antimicrobial polypeptide ε-poly(L-lysine) (ε-PL) was electrostatically incorporated to poly(acrylic acid) (PAA)/poly(vinyl alc.) (PVA) electrospun nanofibers. ε-PL loading and distribution was assessed by IR spectra, ζ-potential measurements and the primary amino reactive dye fluorescamine. Functionalized fibers with 485 ± 140 nm diameter, could be loaded with 0.57-0.74 g ε-PL (g dressing)^-1 that released at a constant rate of 5.4 ± 2.8 mg ε-PL (g dressing day)^-1. Such a dressings resulted in two orders of magnitude lower bacterial colonization than non-functionalized PAA-PVA after 14 days of incubation. Bacterial impairment was attributed to the damage of cell membranes and the formation of intracellular reactive oxygen species. ε-PL functionalized nanofibers did not display cytotoxicity to human corneal epithelial cells, HCEpC, in 24 h MTT assays. However, the viability of rapidly growing tumoral HeLa cells decreased >50% under the same conditions. The prepared biocompatible nanofibrous dressings with durable antibacterial activity show potential application as wound dressings and other biomedical uses. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Category: benzofurans).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Determination of sitagliptin with fluorescamine in tablets and spiked serum samples by spectrofluorimetry and a degradation study was written by Caglar, Sena;Onal, Armagan;Toker, Sidika. And the article was included in Current Pharmaceutical Analysis in 2012.Synthetic Route of C17H10O4 This article mentions the following:

Two novel, simple, and rapid stability-indicating spectrofluorimetric methods were developed for the determination of sitagliptin in tablets and spiked serum samples. In the first method, sitagliptin’s natural fluorescence was measured at 353 nm after excitation at 259 nm. On the basis of the reaction between sitagliptin and fluorescamine the second method was developed in borate buffer solution of pH 9.0 and the fluorescence intensities of the derivatives were measured at 475 nm emission and 390 nm excitation wavelengths. The calibration curves were constructed in concentration range of 0.5-10.0 μg mL^-1 and 0.2-1.4 μg mL^-1 for the first and second method, resp. The developed methods were validated with respect to linearity, precision, sensitivity, accuracy and selectivity. The degradation behavior of the drug was investigated using the first method. The drug solution was subjected to neutral, acid and alkali hydrolysis, oxidation, thermal stress and exposured to the sunlight. The first method is proved to be selective and useful for the investigation of the stability of sitagliptin. The application of spiked serum samples was also analyzed by the second method. The developed methods were successfully applied for the determination of sitagliptin in tablets and spiked serum samples. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Synthetic Route of C17H10O4).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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. 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.Synthetic Route of C17H10O4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Structural Analysis and Aggregation Propensity of Reduced and Nonreduced Glycated Insulin Adducts was written by Alavi, Parnian;Yousefi, Reza;Amirghofran, Sara;Karbalaei-Heidari, Hamid Reza;Moosavi-Movahedi, Ali Akbar. And the article was included in Applied Biochemistry and Biotechnology in 2013.Category: benzofurans This article mentions the following:

The milieu within pancreatic β cells represents a favorable environment for glycation of insulin. Therefore, in this study, insulin samples were individually subjected to glycation under reducing and nonreducing conditions. As monitored by ortho-phthalaldehyde and fluorescamine assays, the reduced glycated insulin adduct demonstrates extensively higher level of glycation than the nonreduced glycated counterpart. Also, gel electrophoresis experiments suggest a significant impact of glycation under a reducing system on the level of insulin oligomerization. Furthermore, reduced and nonreduced glycated insulin adducts resp. exhibit full and partial resistance against dithiothreitol-induced aggregation. The results of thioflavin T and Congo red assays suggest the existence of a significant quantity of amyloid-like entities in the sample of reduced glycated insulin adduct. Both fluorescence and far-UV CD studies resp. suggest that the extents of unfolding and secondary structural alteration were closely correlated to the level of insulin glycation. Moreover, the surface tension of two glycated insulin adducts was inversely correlated to their glycation extents and to the quantity of exposed hydrophobic patches. Overall, the glucose-modified insulin mols. under reducing and nonreducing systems display different structural features having significant consequences on aggregation behaviors and surface tension properties. The particular structural constraints of glycated insulin may reduce the binding interaction of this hormone to its receptor which is important for both insulin function and clearance. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Category: benzofurans).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Functionalization of nano-emulsions with an amino-silica shell at the oil-water interface was written by Attia, Mohamed F.;Anton, Nicolas;Bouchaala, Redouane;Didier, Pascal;Arntz, Youri;Messaddeq, Nadia;Klymchenko, Andrey S.;Mely, Yves;Vandamme, Thierry F.. And the article was included in RSC Advances in 2015.Recommanded Product: 38183-12-9 This article mentions the following:

Nano-emulsions are very promising nano-carriers with high potential for loading lipophilic drugs. However, the surface of oil nano-droplets is a dynamic oil/water interface stabilized by surfactants, and its chem. modification to graft ligands is highly challenging. In this study we developed a new protocol for modification of the nano-droplets surface through a silica shell terminated by amine functions. It enabled preparation of nanocapsules of 65, 85 and 120 nm diameters with a surface coverage of ca. 2 amino groups per nm². The nanocapsule surface was then functionalized (41% efficiency) by a model fluorescent ligand (coumarin blue) with a carboxylic function. The evidence for the successful grafting was provided by spectrofluorometry, Förster resonance energy transfer, at. force microscopy coupled with fluorescence imaging and fluorescence correlation spectroscopy. This simple protocol for surface functionalization of the liquid/liquid interface of lipid droplets may constitute a real advance regarding potential applications that need efficient decoration of droplets with ligands. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Recommanded Product: 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Recommanded Product: 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ring Opening Metathesis Polymerization of Bicyclic α,β-Unsaturated Anhydrides for Ready-to-be-grafted Polymers Having Tailored pH-Responsive Degradability was written by Kim, Heejin;Kim, Sungwhan;Kang, Sunyoung;Song, Youngjun;Shin, Suyong;Lee, Seonju;Kang, Minji;Nam, So Hee;Lee, Yan. And the article was included in Angewandte Chemie, International Edition in 2018.HPLC of Formula: 38183-12-9 This article mentions the following:

Polymers having α,β-unsaturated anhydrides as repeating units were synthesized by ring opening metathesis polymerization (ROMP). The anhydride moieties were ready-to-be-grafted with amines to form acid-labile cis-α,β-unsaturated acid amide linkages. The pH-responsive reversible de-grafting can be controlled by changing the intramol. accessibility between acid and amide groups. The alendronate-grafted ROMP polymers showed distinct pH-dependent cytotoxicity according to the anhydride structures. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9HPLC of Formula: 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) 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.HPLC of Formula: 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem