Tag: M.W=150-200

Fujikura, Takashi published the artcileStudies on benzenesulfonamide derivatives with α- and β-adrenergic antagonistic and antihypertensive activities, Computed Properties of 35203-88-4, the main research area is benzenesulfonamide sympatholytic antihypertensive preparation; aminoethylbenzenesulfonamide phenylmethylpropyl; phenoxyethylaminoethylbenzenesulfonamide; structure activity benzenesulfonamide aminohydroxyethyl.

New α- and β-adrenergic blockers, benzenesulfonamide derivatives I (R = H, halo, MeO, Me, Pr, MeS, MeSO2; R1 = H, MeO) and II (R2 = Me, MeO, OH; R3 = H, OH, MeO, EtO) were prepared from acetylbenzenesulfonamides. All the target compounds have two asym. centers and therefore consist of two diastereomers. I (R = 2-Me, R1 = 2-MeO) (III) and II (R2 = Me, R3 = 2-MeO) (IV) showed potent α- and β-blocking activities and they were each separated into two diastereomers (III-A and III-B, and IV-A and IV-B) and one isomer had mainly β-blocking activity and the other isomer had mainly α-blocking activity. In addition, several compounds showing relatively strong α- and β-blocking activities were also examined for antihypertensive activity and III and IV were more potent than labetalol. Structure-activity relationships were discussed.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Computed Properties of 35203-88-4.

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

Zayas-Gonzalez, Yashira M. published the artcileDegradable Amine-Reactive Coatings Fabricated by the Covalent Layer-by-Layer Assembly of Poly(2-vinyl-4,4-dimethylazlactone) with Degradable Polyamine Building Blocks, SDS of cas: 10405-38-6, the main research area is amine reactive coating fabricated covalent assembly polyvinyldimethylazlactone polyamine.

We report the fabrication of reactive and degradable crosslinked polymer multilayers by the reactive/covalent layer-by-layer assembly of a non-degradable azlactone-functionalized polymer [poly(2-vinyl-4,4-dimethylazlactone), PVDMA] with hydrolytically or enzymically degradable polyamine building blocks. Fabrication of multilayers using PVDMA and a hydrolytically degradable poly(β-amino ester) (PBAE) containing primary amine side chains yielded multilayers (∼100 nm thick) that degraded over ∼12 days in physiol. relevant media. Physicochem. characterization and studies on stable films fabricated using PVDMA and an analogous non-degradable poly(amidoamine) suggested that erosion occurred by chem. hydrolysis of backbone esters in the PBAE components of these assemblies. These degradable assemblies also contained residual amine-reactive azlactone functionality that could be used to impart new functionality to the coatings post-fabrication. Crosslinked multilayers fabricated using PVDMA and the enzymically degradable polymer poly(L-lysine) were structurally stable for prolonged periods in physiol. media, but degraded over ∼24 h when the enzyme trypsin was added. Past studies demonstrate that multilayers fabricated using PVDMA and non-degradable polyamines [e.g., poly(ethyleneimine)] enable the design and patterning of useful nano/bio-interfaces and other materials that are structurally stable in physiol. media. The introduction of degradable functionality into PVDMA-based multilayers creates opportunities to exploit the reactivity of azlactone groups for the design of reactive materials and functional coatings that degrade or erode in environments that are relevant in biomedical, biotechnol., and environmental contexts. This ‘degradable building block’ strategy should be general; we anticipate that this approach can also be extended to design of amine-reactive multilayers that degrade upon exposure to specific chem. triggers, selective enzymes, or contact with cells by judicious design of the degradable polyamine building blocks used to fabricate the coatings.

Biomacromolecules published new progress about Coating materials. 10405-38-6 belongs to class amides-buliding-blocks, name is N,N’-(Butane-1,4-diyl)diacrylamide, and the molecular formula is C10H16N2O2, SDS of cas: 10405-38-6.

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

Hochstrasser, Denis F. published the artcileDevelopment of polyacrylamide gels that improve the separation of proteins and their detection by silver staining, Recommanded Product: N,N’-(Butane-1,4-diyl)diacrylamide, the main research area is protein separation gel electrophoresis crosslinker; silver staining protein detection crosslinker.

Background staining that is associated with Ag detection of proteins and nucleic acids in polyacrylamide gels was due mostly to the amide groups in methylenebisacrylamide, a commonly used gel crosslinker. To reduce this background staining, 8 existing crosslinking agents were tested; all were unsuitable. Six new crosslinking agents were synthesized and tested. Of these, diacrylylpiperazine provided increased phys. strength, improved electrophoretic separation of proteins, and Ag staining detection of proteins with reduced background stain.

Analytical Biochemistry published new progress about Biological staining. 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

Mohammad, Haroon published the artcileDiscovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus, COA of Formula: C11H15NS, the main research area is thiazole antibacterial Staphylococcus antibiotic resistance.

Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA) infections are growing global health concerns. Structure-activity relationships of phenylthiazoles as a new antimicrobial class have been addressed. The authors present 10 thiazole derivatives that exhibit strong activity against 18 clin. strains of MRSA and VRSA with acceptable PK profile. Three derivatives revealed an advantage over vancomycin by rapidly eliminating MRSA growth within 6 h, and no derivatives are toxic to HeLa cells at 11 μg/mL.

Journal of Medicinal Chemistry published new progress about Antibacterial 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

Seleem, Mohammed A. published the artcileSecond-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties, Safety of 4-Butylthiobenzamide, the main research area is methicillin resistant Staphylococcus aureus antibacterial phenylthiazole preparation; thiazole phenyl preparation methicillin resistant Staphylococcus aureus antibacterial.

A series of second-generation analogs for 2-(1-(2-(4-butylphenyl)-4-methylthiazol-5-yl)ethylidene)aminoguanidine have been synthesized and tested against methicillin-resistant Staphylococcus aureus (MRSA). The compounds were designed with the objective of improving pharmacokinetic properties. This main aim has been accomplished by replacing the rapidly hydrolyzable Schiff-base moiety of first-generation members with a cyclic, unhydrolyzable pyrimidine ring. The hydrazide-containing analog I was identified as the most potent analog constructed thus far. The corresponding amine was 8 times less active. Finally, incorporating the nitrogenous side chain within an aromatic system completely abolished the antibacterial character. Replacement of the Bu group with cyclic bioisosteres revealed cyclohexenyl analog II, which showed significant improvement in in vitro anti-MRSA potency. Increasing or decreasing the ring size deteriorated the antibacterial activity. Compound I demonstrated a superior in vitro and in vivo pharmacokinetic profile, providing compelling evidence that this particular analog is a good drug candidate worthy of further anal.

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Safety of 4-Butylthiobenzamide.

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

Mayhoub, Abdelrahman S. published the artcileOptimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1), Quality Control of 1208077-46-6, the main research area is resveratrol thiazole analog preparation NADPH quinone reductase structure cancer.

NAD(P)H:quinone reductase 1 (QR1) belongs to a class of enzymes called cytoprotective enzymes. It exhibits its cancer protective activity mainly by inhibiting the formation of intracellular semiquinone radicals, and by generating α-tocopherolhydroquinone, which acts as a free radical scavenger. It is therefore believed that QR1 inducers can act as cancer chemopreventive agents. Resveratrol (1) is a naturally occurring stilbene derivative that requires a concentration of 21 μM to double QR1 activity (CD = 21 μM). The stilbene double bond of resveratrol was replaced with a thiadiazole ring and the phenols were eliminated to provide a more potent and selective derivative 2 (CD = 2.1 μM). Optimizing the substitution pattern of the two Ph rings and the central heterocyclic linker led to a highly potent and selective QR1 inducer 9o with a CD value of 0.087 μM.

Bioorganic & Medicinal Chemistry published new progress about Anti-inflammatory agents. 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Quality Control of 1208077-46-6.

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

Carotti, Angelo published the artcileInhibition of carbonic anhydrase by substituted benzenesulfonamides. A reinvestigation by QSAR and molecular graphics analysis, Computed Properties of 35203-88-4, the main research area is carbonic anhydrase inhibitor benzenesulfonamide QSAR.

The inhibition of bovine carbonic anhydrase B by an appropriately designed set of m- and p-substituted benzenesulfonamides (I, R = H, halo, alkoxy, aryl, etc.) was studied. From the results the following quant. structure-activity relationship was derived: log 1/Ki = 0.95σ + 0.54π – 0.35B5,3 + 6.29. In this equation Ki is the inhibition constant, σ is the Hammett constant, π is the hydrophobic parameter and B5,3 is the sterimol steric parameter for the m-substituents. Using this equation, a new congener was designed and synthesized and the Ki for a new congener intended to maximize the inhibitory potency (1/Ki) was predicted. The interactions involved in the enzyme-inhibitors binding as suggested by the correlation equation, have been tentatively interpreted using computer built 3-D mol. models based on the published X-ray crystallog. coordinates of the free and inhibitor-bound carbonic anhydrase. The results from our analyses have been compared with those obtained in some previous QSAR analyses.

Quantitative Structure-Activity Relationships published new progress about Arenesulfonamides Role: USES (Uses). 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Computed Properties of 35203-88-4.

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

Wang, Zi-Qiang published the artcileElectrochemical Synthesis of 3,5-Disubstituted-1,2,4-thiadiazoles through NH4I-Mediated Dimerization of Thioamides, Recommanded Product: 4-Butylthiobenzamide, the main research area is thiadiazole disubstituted preparation electrochem; thioamide oxidative dimerization ammonium iodide electrolyte catalyst.

A electrochem. method for the synthesis of 3,5-disubstituted-1,2,4-thiadiazoles through NH4I-mediated dimerization of thioamides is reported. Using the inexpensive NH4I as electrolyte and catalyst, this electrosynthesis approach requires no oxidizing agents and enables the convenient production of diverse 1,2,4-thiadiazole products. The approach is an example of S-N bond construction through the electrochem. method.

Advanced Synthesis & Catalysis published new progress about Bond formation (sulfur-nitrogen). 1208077-46-6 belongs to class amides-buliding-blocks, name is 4-Butylthiobenzamide, and the molecular formula is C11H15NS, Recommanded Product: 4-Butylthiobenzamide.

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

Ohkubo, Katsutoshi published the artcileShape- and stereo-selective esterase activities of cross-linked polymers imprinted with a transition-state analogue for the hydrolysis of amino acid esters, Recommanded Product: N,N’-(Butane-1,4-diyl)diacrylamide, the main research area is nitrophenyl leucinate hydrolysis kinetics polymeric catalyst; histidyl polymer preparation catalyst hydrolysis leucinate; isokinetic relationship catalytic hydrolysis nitrophenyl leucinate.

Various cross-linked (with N,N’-ethylene (C2), butylene (C4), hexamethylene (C6), or decamethylene (C10)-bisacrylamide) polymer catalysts containing L-histidine and quaternary trimethylammonium groups were imprinted with a racemic transition-state analog of Ph 1-benzyloxycarbonyl-3-methylpentylphosphonate for the hydrolysis of p-nitrophenyl N-(benzyloxycarbonyl)-L (or D)-leucinate [Z-L (or D)-Leu-PNP]. Among these polymer catalysts, N,N’-C4-bisacrylamide-cross-linked polymer catalyst, which was copolymerized with styrene monomer, exhibited notable substrate-stereospecificity for the Z-L-Leu-PNP hydrolysis in the hydrolysis of enantiomeric L (or D)-N-protected [such as tert-butyloxycarbonyl (Boc-), acetyl (C2-), decanoyl (C10-) or benzyloxycarbonyl (Z-)] amino acid (Leu, Ala, or Phe) p-nitrophenyl esters in 10 volume % MeCN-Tris buffer (pH 7.15) at 30°C.

Journal of Molecular Catalysis A: Chemical published new progress about Amino acid esters Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Dong, Yi published the artcileRhodium(III)-catalyzed sulfonamide directed ortho C-H carbenoid functionalization via metal carbene migratory insertion, HPLC of Formula: 35203-88-4, the main research area is diazoacetate arylsulfonyl acetamide preparation rhodium catalyst regioselective migratory insertion; acetylsulfamoyl arylacetate preparation.

A rhodium(III)-catalyzed sulfonamide directed ortho C-H carbenoid functionalization was developed with good yields. This method was attractive due to its broad substrate scope and enabled derivation of diverse biol. active sulfonamide structures and late-stage modification of sulfa drugs.

Chemical Communications (Cambridge, United Kingdom) published new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, HPLC of Formula: 35203-88-4.

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