Category: 1208077-46-6

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

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

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

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

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