391906-08-4

Upstream product

• 51746-82-8 2-amino-1-pyridin-3-yl-ethanone dihydrochloride salt 
• 500-22-1 3-pyridinecarboxaldehyde 
• 57402-97-8 N-<(trimethylsilyl)methyl>benzaldimine 
• 350-03-8 methyl-3-pyridylketone 
• 6283-81-4 3-oxo-3-pyridin-3-yl-propionic acid ethyl ester 
• 800402-00-0 2-(2-oxo-2-pyridin-3-yl-ethyl)-isoindole-1,3-dione 
• 101861-30-7 rac-2-nitro-1-(pyridin-3-yl)ethan-1-ol 
• 174060-40-3 3-[(2R)-oxiranyl]pyridine 
• 329281-07-4 (S)-3-(2-oxiranyl)pyridine 
• 17694-68-7 3-(2-bromoacetyl)pyridine hydrobromide 
• 391906-07-3 (1R)-2-bromo-1-(3-pyridinyl)-1-ethanol 
• 6221-12-1 3-Bromoacetylpyridine 
• 61296-12-6 2-hydroxyimino-3-oxo-3-[3]pyridyl-propionic acid ethyl ester 
• 92639-84-4 2-hydroxyimino-1-(3-pyridyl)-1-ethanone 

Relevant academic research and scientific papers

Novel amide- and sulfonamide-based aromatic ethanolamines: Effects of various substituents on the inhibition of acid and neutral ceramidases

In the present study we describe the design and synthesis of a series of amide- and sulfonamide-based compounds as inhibitor of recombinant acid and neutral ceramidases. Inhibition of ceramidases has been shown to induce apoptosis and to increase the efficacy of conventional chemotherapy in several cancer models. B-13, lead in vitro inhibitor of acid ceramidase has been recently shown to be virtually inactive towards lysosomal acid ceramidase in living cells at lower concentrations and for a shorter time of treatment, suggesting the development of more potent inhibitors. In this study, a detailed SAR investigation has been performed to understand the effect of different substituents on the phenyl ring of amide- and sulfonamide-based compounds that partially resemble the structure of well-known inhibitors such as B-13, D-e-MAPP as well as NOE. Our results suggest that the electronic effects of the substituents on phenyl ring in B-13 and D-e-MAPP analogues have negligible effects either in enhancing the inhibition potencies or for selectivity towards aCDase over nCDase. However, the hydrophobicity and the steric effects of longer alkyl chains (n-Pr, n-Bu or t-Bu groups) at the phenyl ring were found to be important for an enhanced selectivity towards aCDase over nCDase.

INDOLE-2-CARBOXYLIC ACID AMIDES

Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or

PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE

Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.

2,4-Thiazolidinediones as potent and selective human β3 agonists

Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50 = 0.01 μM, IA = 1.19) and selective (more than 110-fold over β1 and β2 agonist activity) β3 agonist. This compound has also been proven to be active and selective in an in vivo mode.

Synthetic Versatility of N(Silylmethyl)imines: Water-Induced Generation of N-Protonated Azomethine Ylides of Nonstabilized Type and Fluoride-Induced Generation of 2-Azallyl Anions

N-(Silylmethyl)imines generate N-protonated azomethine ylides of nonstabilized type when treated with water in HMPA, which undergo stereospecific and regioselective cycloadditions with electron-poor olefins affording N-unsubstituted pyrrolidines.On the other hand, fluoride-induced desilylation of the imines leads to 2-azallyl anions which are found to be synthetic equivalents of aminomethyl anion in the Michael additions with electron-poor olefins and nucleophilic additions with carbonyl compounds.