104857-27-4

Upstream product

• 139356-43-7 2-(2-Methyl-propane-2-sulfinyl)-N-phenyl-nicotinamide 
• 104857-35-4 2,2'-dithiobis 
• 62-53-3 aniline 
• 56149-29-2 2-chloro-N-phenylpyridine-3-carboxamide 
• 38521-46-9 3-carboxy-2-mercaptopyridine 
• 104857-34-3 2,2'-dithiobis(3-pyridinecarbonyl chloride) 
• 112811-90-2 2-benzylsulfanylnicotinic acid 
• 104857-16-1 N-(phenyl)-1,2-dihydro-2-thioxo-3-pyridinecarboxamide 
• 139356-44-8 N-Phenyl-2-phenylmethanesulfinyl-nicotinamide 

Downstream Products

• 13222-85-0 p-methylbenzoic anhydride 
• 104857-16-1 N-(phenyl)-1,2-dihydro-2-thioxo-3-pyridinecarboxamide 

Relevant academic research and scientific papers

REDOX DEHYDRATION COUPLING CATALYSTS AND METHODS RELATED THERETO

This disclosure relates to synthetic coupling methods using catalytic molecules. In certain embodiments, the catalytic molecules comprise heterocyclic thiolamide, S-acylthiosalicylamide, disulfide, selenium containing heterocycle, diselenide compound, ditelluride compound or tellurium containing heterocycle. Catalytic molecules disclosed herein are useful as catalysts in the transformation of hydroxy group containing compounds to amides, esters, ketones, and other carbon to heteroatom or carbon to carbon transformations.

Benzoisothiazolone organo/copper-cocatalyzed redox dehydrative construction of amides and peptides from carboxylic acids using (EtO)3P as the reductant and O2 in air as the terminal oxidant

Carboxylic acids and amine/amino acid reactants can be converted to amides and peptides at neutral pH within 5-36 h at 50 °C using catalytic quantities of a redox-active benzoisothiazolone and a copper complex. These catalytic "oxidation-reduction condensation" reactions are carried out open to dry air using O2 as the terminal oxidant and a slight excess of triethyl phosphite as the reductant. Triethyl phosphate is the easily removed byproduct. These simple-to-run catalytic reactions provide practical and economical procedures for the acylative construction of C-N bonds.

A novel kind of dimmer (excimer)-induced-AIE compound 2- phenylisothiazolo[5,4-b]pyridin-3(2H)-one as high selective bisulfite anion probe

An interesting dimmer (excimer)-induced-AIE characteristic of 2-phenylisothiazolo[5,4-b]pyridin-3(2H)-one was observed. By using a ring-opening reaction, we developed a novel fluorescent probe based on sub-micron particles of 2-phenylisothiazolo[5,4-b]pyridin-3(2H)-one in water.

Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors

We present a combination of database screening, synthesis and in vitro testing to identify novel histone acetyltransferase (HAT) inhibitors. The National Cancer Institute compound collection (NCI) and several commercial databases were filtered by similarity-based virtual screening to find new HAT inhibitors. Employing the recombinant HAT p300/CBP-associated factor (PCAF) and two different histone substrates for screening, pyridoisothiazolones were identified as inhibitors of human PCAF. Due to the limited solubility of the initial hits, we synthesized and tested them on PCAF. The compounds inhibit the proliferation of cancer cells. In summary, valuable chemical tools and potential lead candidates for new anticancer agents directed against HATs as new targets have been identified.

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs)

High-throughput screening led to the identification of isothiazolones 1 and 2 as inhibitors of histone acetyltransferase (HAT) with IC50s of 3 μM and 5 μM, respectively. Analogues of these hit compounds with variations of the N-phenyl group, and with vari

Heteroaryl-Fused 2-Phenylisothiazolone Inhibitors of Cartilage Breakdown

The synthesis, biological evaluation, and structure-activity relationships of a series of N-phenyl heteroaryl-fused isothiazolones are described.These isothiazolones have been shown to exhibit potent, dose-dependent inhibition of IL-1β-induced breakdown of proteoglycan in a cartilage organ culture assay.This effect is likely due to inhibition of MMP activation and a consequent reduction in MMP activity following IL-1β stimulation.Thus these compounds potentially represent simple, non-peptidic disease-modifying agents for the treatment of arthritic diseases.To examine the effects of structure on in vitro activity, three general features of the molecules were varied, substituents on the pendant N-phenyl group, the position of ring fusion to the isothiazolone, and substituents on the fused ring peri to the isothiazolone sulfur.

Benzyl and t-butyl sulfoxides as sulfenyl halide equivalents: A convenient preparation of benzisothiazolones

A new methodology is described for the synthesis of benzisothiazolones from benzylsulfinyl or t-butylsulfinyl substituted carboxamides that provides a mild alternative to conventional cyclization methods that employ halogens.