Tag: M.W=150-200

Mayhoub, Abdelrahman S. published the artcileOptimizing thiadiazole analogues of resveratrol versus three chemopreventive targets, Synthetic Route of 1208077-46-6, the main research area is resveratrol thiadiazole analog preparation antitumor aromatase NFkappaB QR1.

Chemoprevention is an approach to decrease cancer morbidity and mortality through inhibition of carcinogenesis and prevention of disease progression. Although the trans stilbene derivative resveratrol has chemopreventive properties, its action is compromised by weak non-specific effects on many biol. targets. Replacement of the stilbene ethylenic bridge of resveratrol with a 1,2,4-thiadiazole heterocycle and modification of the substituents on the two aromatic rings afforded potential chemopreventive agents with enhanced potencies and selectivities when evaluated as inhibitors of aromatase and NF-κB and inducers of quinone reductase 1 (QR1).

Bioorganic & Medicinal Chemistry published new progress about Antioxidants. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Synthetic Route of 1208077-46-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Lee, S. K. published the artcileTemperature dependence of the binding of methyl orange by crosslinked poly(4-vinylpyridine), Formula: C10H16N2O2, the main research area is vinylpyridine polymer binding methyl orange; crosslinking vinylpyridine polymer dye binding.

The title polymers with different degrees of crosslinking were prepared by radical copolymerization of 4-vinylpyridine with 3-20% N,N’-tetramethylenebisacrylamide. The binding abilities of these crosslinked polymers with methyl orange were investigated at various temperatures in a buffer solution of pH 7. The first binding constant (K1) and thermodn. parameters were evaluated from the equilibrium amounts of binding. K1 showed bell-shaped curves when plotted against both the binding temperature and the degree of crosslinking. Lower temperature and higher degree of crosslinking at maximum binding in these bell-shaped curves were observed for this binding system when compared with those in a system using N,N’-methylenebisacrylamide as crosslinker. The values of the enthalpy and entropy change increased on increasing the degree of crosslinking and decreasing the binding temperature, whereas the absolute magnitude of the free-energy change was not increased. These results could be accounted for in terms of the temperature dependence of the hole size of the crosslinked polymers in addition to the hydrophobic interactions in the binding process.

Polymer published new progress about Crosslinking. 10405-38-6 belongs to class amides-buliding-blocks, name is N,N’-(Butane-1,4-diyl)diacrylamide, and the molecular formula is C10H16N2O2, Formula: C10H16N2O2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Hong, W. David published the artcileAWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, COA of Formula: C7H5F3N2O, the main research area is AWZ1066S antibacterial antifilarial pharmacokinetics toxicity Wolbachia filariasis; anti-Wolbachia; drug discovery; lymphatic filariasis; macrofilaricide; onchocerciasis.

Onchocerciasis and lymphatic filariasis are two neglected tropical diseases that together affect ∼ 157 million people and inflict severe disability. Both diseases are caused by parasitic filarial nematodes with elimination efforts constrained by the lack of a safe drug that can kill the adult filaria (macrofilaricide). Previous proof-of-concept human trials have demonstrated that depleting > 90% of the essential nematode endosymbiont bacterium, Wolbachia, using antibiotics, can lead to permanent sterilization of adult female parasites and a safe macrofilaricidal outcome. AWZ1066S is a highly specific anti-Wolbachia candidate selected through a lead optimization program focused on balancing efficacy, safety and drug metabolism/pharmacokinetic (DMPK) features of a thienopyrimidine/quinazoline scaffold derived from phenotypic screening. AWZ1066S shows superior efficacy to existing anti-Wolbachia therapies in validated preclin. models of infection and has DMPK characteristics that are compatible with a short therapeutic regimen of 7 days or less. This candidate mol. is well-positioned for onward development and has the potential to make a significant impact on communities affected by filariasis.

Proceedings of the National Academy of Sciences of the United States of America published new progress about Anthelmintics. 959108-47-5 belongs to class amides-buliding-blocks, name is 2-(Trifluoromethyl)nicotinamide, and the molecular formula is C7H5F3N2O, COA of Formula: C7H5F3N2O.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Jacobs, Jeffrey W. published the artcileDiscovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na+/H+ Exchanger Isoform 3, SDS of cas: 35203-88-4, the main research area is tenapanor inhibitor intestine sodium hydrogen exchanger isoform 3 NHE3.

We present herein the design, synthesis, and optimization of gut-restricted inhibitors of Na+/H+ exchanger isoform 3 (NHE3). NHE3 is predominantly expressed in the kidney and gastrointestinal tract where it acts as the major absorptive sodium transporter. We desired minimally systemic agents that would block sodium absorption in the gastrointestinal tract but avoid exposure in the kidney. Starting with a relatively low-potency highly bioavailable hit compound (1), potent and minimally absorbed NHE3 inhibitors were designed, culminating with the discovery of tenapanor (28). Tenapanor has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of irritable bowel syndrome with constipation in adults.

ACS Medicinal Chemistry Letters published new progress about Digestive tract. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, SDS of cas: 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Galley, W. C. published the artcileKinetics of triplet-triplet energy transfer and intramolecular distances in enzyme-inhibitor complexes, Formula: C8H9NO3S, the main research area is kinetics energy transfer bimol; enzyme inhibitor complex conformation; mol distance energy transfer.

The kinetics of triplet-triplet energy transfer and donor-acceptor geometries were used to estimate mol. distances in bimol. systems and to measure variability within enzyme-inhibitor complexes. The average distance from the center of the energy donor (m-acetylbenzene sulfonamide) to that of ≥1 tryptophan residue in bovine, human B, and human C forms of carbonic anhydrase were estimated as 10.1, <9.5, and 10.4 Å, resp. The use of kinetics of triplet energy transfer is recommended for studying bimol. conformations. Nature (London, United Kingdom) published new progress about Energy transfer. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Formula: C8H9NO3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

McCarville, Michael published the artcilePhosphorescent probes for proteins, Quality Control of 35203-88-4, the main research area is carbonic anhydrase inhibitor phosphorescent; tryptophan energy transfer; protein phosphorescent probes.

Use of bound phosphorescent chromophores to study protein structure was investigated. Carbonic anhydrase inhibitors with 3 different arrangements of singlet and triplet energy levels relative to those of tryptophan were used to determine their ability to transfer triplet energy. Ligands representing each of the 3 energy level arrangements were found to exhibit triplet-triplet energy transfer with a tryptophan residue at the active site of carbonic anhydrase. This greatly increases the number of ligands which may be useful as phosphorescent probes and is a potential source of data for determining the position of the ligand in the binding site.

Biochimica et Biophysica Acta, Protein Structure published new progress about Energy transfer. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Quality Control of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Boskovic, Zarko V. published the artcileSynthesis of piperlogs and analysis of their effects on cells, Related Products of amides-buliding-blocks, the main research area is piperlog preparation antitumor structure activity; reactive oxygen species level piperlog; piperlongumine analog preparation antitumor structure activity; Michael acceptors; piperlongumine; reactive oxygen species; toxicity.

Piperlongumine (PL) (I) is a naturally occurring small mol. previously shown to induce cell death preferentially in cancer cells relative to non-cancer cells. An initial effort to synthesize analogs highlighted the reactivities of both of piperlongumine’s α,β-unsaturated imide functionalities as key features determining PL’s cellular effects. In this study, a second-generation of analogs, e.g., II, was synthesized and evaluated in cells to gain further insight into how the reactivity, number, and orientation of PL’s reactive olefins contribute to its ability to alter the physiol. of cells.

Tetrahedron published new progress about Antitumor agents. 10405-38-6 belongs to class amides-buliding-blocks, name is N,N’-(Butane-1,4-diyl)diacrylamide, and the molecular formula is C10H16N2O2, Related Products of amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mayhoub, Abdelrahman S. published the artcileAn investigation of phenylthiazole antiflaviviral agents, COA of Formula: C11H15NS, the main research area is antiflaviviral phenylthiazole preparation SAR.

Flaviviruses are one of the most clin. important pathogens and their infection rates are increasing steadily. The phenylthiazole ring system has provided a template for the design and synthesis of antiviral agents that inhibit the flaviviruses by targeting their E-protein. Unfortunately, there is a correlation between phenylthiazole antiflaviviral activity and the presence of the reactive and therefore potentially toxic mono- or dibromomethyl moieties at thiazole-C4. Adding a linear hydrophobic tail para to the Ph ring led to a new class of phenylthiazole antiflaviviral compounds that lack the toxic dibromomethyl moiety. This led to development of a drug-like phenylthiazole 12 (I) that had high antiflaviviral selectivity (TI = 147).

Bioorganic & Medicinal Chemistry published new progress about Antiviral agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, COA of Formula: C11H15NS.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Moszner, Norbert published the artcileMonomers for adhesive polymers, 4 synthesis and radical polymerization of hydrolytically stable crosslinking monomers, Recommanded Product: N,N’-(Butane-1,4-diyl)diacrylamide, the main research area is dentin adhesive bisacrylamide monomer.

Hydrolytically stable, crosslinking bis(acrylamide)s 1a-1l or bis(methacrylamide)s 2a-2c were synthesized by reaction of acryloyl or methacryloyl chloride using primary or secondary amines. In addition, monomers 3a and 3b were obtained by amidation of 2,6-dimethylene-4-oxaheptane-1,7-dicarboxylic acid (DMOHDA) with propylamine and diethylamine, resp. The structures of the monomers were characterized by IR, 1H, and 13C NMR spectroscopy. All monomers containing N,N’-monosubstituted carbamide groups were solids. Those containing N,N’-disubstituted carbamide groups were water-soluble liquids Water-soluble bis(acrylamide) 1d (N,N’-diethyl-1,3-bis(acrylamido)propane) shows a radical polymerization reactivity in the presence of 2,2′-azobis(2-methylpropionamidine) dihydrochloride (AMPAHC) similar to that of glycerol dimethacrylate, as revealed by gelation experiments in water. 1D is hydrolytically stable in 20 weight-% phosphoric acid and can be used to substitute dimethacrylates in self-etching dentin adhesives. Furthermore, this monomer was also suitable as a reactive diluent in composites.

Macromolecular Materials and Engineering published new progress about Bending strength. 10405-38-6 belongs to class amides-buliding-blocks, name is N,N’-(Butane-1,4-diyl)diacrylamide, and the molecular formula is C10H16N2O2, Recommanded Product: N,N’-(Butane-1,4-diyl)diacrylamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Tong, Wei published the artcilePalladium-Metalated Porous Organic Polymers as Recyclable Catalysts for the Chemoselective Synthesis of Thiazoles from Thiobenzamides and Isonitriles, Application of 4-Butylthiobenzamide, the main research area is thiobenzamide isonitrile polymer supported palladium catalyst cascade; thiazole derivative chemoselective preparation; isonitrile thiobenzamide polymer supported palladium catalyst cascade cyclization; imidazothiazole chemoselective preparation anticancer activity.

Two types of thiazole derivatives are synthesized through a multistep cascade sequence with Pd-metalated phosphorus-doped porous organic polymers (POPs) as heterogeneous catalysts. The POPs could be used as both ligands and catalyst supports. No obvious aggregation and loss of any catalytic activity of the catalysts were observed after 10 runs of the reaction. More importantly, imidazo[4,5-d]thiazoles, which are a new class of thiazole derivatives, could be obtained through K2CO3-promoted intramol. cyclization of the synthesized polysubstituted thiazoles. Furthermore, the in vitro anticancer activity of these new compounds were tested with MTT assay, and compound I exhibited good antitumor activity toward T-24 and A549 cells with IC50 values of 10.3 ± 0.8 and 11.8 ± 0.5 μM, resp. In addition, the action mechanism of compound I on tumor cells was determined

Organic Letters published new progress about Antitumor agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Application of 4-Butylthiobenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics