91859-66-4

Upstream product

• 139356-49-3 N-Benzyl-2-phenylmethanesulfinyl-nicotinamide 
• 91859-79-9 N-Benzyl-2-mercapto-nicotinamide 
• 65282-42-0 1,2-dithiolo<5,4-b>pyridin-3-one 
• 100-39-0 benzyl bromide 
• 52505-45-0 2-mercaptopyridine-3-carbonitrile 
• 6602-54-6 2-chloro-3-pyridinecarbonitrile 
• 50596-67-3 2-mercapto-3-pyridinecarboxamide 
• 4337-60-4 isothiazolo[5,4-b]pyridin-3(2H)-one 
• 38521-46-9 3-carboxy-2-mercaptopyridine 
• 330667-57-7 2-mercapto-N-pentyl-nicotinamide 
• 154344-33-9 2-phenylethylisothiazolo<5,4-b>pyridine-3(2H)-thione 
• 154344-45-3 2-phenethylisothiazolo<5,4-b>pyridin-3(2H)-one 
• 154344-30-6 2-pentylisothiazolo<5,4-b>pyridine-3(2H)-thione 
• 154344-43-1 2-pentylisothiazolo<5,4-b>pyridin-3(2H)-one 

Downstream Products

• 154344-32-8 2-benzylisothiazolo<5,4-b>pyridine-3(2H)-thione 
• 154344-26-0 N-Benzyl-2-mercapto-thionicotinamide 
• 154344-28-2 2-Mercapto-N-(3-phenyl-propyl)-thionicotinamide 
• 154344-33-9 2-phenylethylisothiazolo<5,4-b>pyridine-3(2H)-thione 
• 154344-27-1 2-Mercapto-N-phenethyl-thionicotinamide 
• 154344-46-4 2-(3-phenylpropyl)isothiazolo<5,4-b>pyridin-3(2H)-one 
• 154344-34-0 2-(3-phenylpropyl)isothiazolo<5,4-b>pyridine-3(2H)-thione 
• 330667-58-8 2-mercapto-N-phenethyl-nicotinamide 
• 330667-59-9 2-mercapto-N-(3-phenyl-propyl)-nicotinamide 
• 65282-42-0 1,2-dithiolo<5,4-b>pyridin-3-one 
• 3445-78-1 3H-1,2-dithiolo<3,4-b>pyridine-3-thione 

Relevant academic research and scientific papers

Bioisosteric investigation of ebselen: Synthesis and in vitro characterization of 1,2-benzisothiazol-3(2H)-one derivatives as potent New Delhi metallo-β-lactamase inhibitors

Carbapenem-resistant Enterobacteriaceae (CRE) producing New Delhi metallo-β-lactamase (NDM-1) cause untreatable bacterial infections, posing a significant threat to human health. In the present study, by employing the concept of bioisosteric replacement of the selenium moiety of ebselen, we have designed, synthesized and characterized a small compound library of 2-substituted 1,2-benzisothiazol-3(2H)-one derivatives and related compounds for evaluating their cytotoxicity and synergistic activity in combination with meropenem against the E. coli Tg1 (NDM-1) strain. The most promising compound 3a demonstrated potent synergistic activity against a panel of clinically isolated NDM-1 positive CRE strains with FICI as low as 0.09. Moreover, its IC50 value and inhibition mechanism were also confirmed by using the enzyme inhibition assay and the ESI-MS analysis respectively. Importantly, compound 3a has acceptable toxicity and is not a PAINS. Because of its structural simplicity and potent synergistic activity in combination with meropenem, we propose that compound 3a may be a promising meropenem adjuvant and a new series of such compounds may worth further investigations.

1,2-BENZISOSELENAZOL-3(2H)-ONE AND 1,2-BENZISOTHIAZOL-3(2H)-ONE DERIVATIVES AS BETA-LACTAM ANTIBIOTIC ADJUVANTS

Provided herein are compositions and methods useful in the treatment of beta-lactam antibiotic resistant bacteria.

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.

3H-[1,2]Dithiolo[3,4-b]pyridine-3-thione and its derivatives. Synthesis and antimicrobial activity

A series of 2-substituted isothiazolo[5,4-b]pyridine-3(2H)-thiones, isothiazolo[5,4-b]pyridin-3(2H)-ones, N-substituted 2-sulfanylnicotinamides and the corresponding carbothioamide derivatives were synthesized and evaluated for their antimicrobial activity against several strains of Gram+ and Gram-bacteria and fungi. Chemical syntheses were resumed into a comprehensive cyclic route that enables the reversible conversion for each derivative of the series considered. Among the tested compounds the N-(aralkyl)-2-sulfanylnicotinamides show the highest fungitoxicity (MIC=1.25-5 μg/ml). The best activity towards Gram-positive bacteria was in the range of 2.5-5 μg/ml. Activity against Gram-negative bacteria was generally very poor for all compounds. Copyright

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.