147283-78-1

Usage

Classification

Organic acid, nitro derivative of oxopyridine

Uses

Building block in the synthesis of biologically active compounds, potential use in pharmaceuticals and agrochemicals

Properties

Antimicrobial, anti-inflammatory

Potential risks

Health hazards, environmental risks due to nitro group

Precautions

Caution should be exercised in handling and use.

Upstream product

• 6332-56-5 3-nitropyridone 
• 79-11-8 chloroacetic acid 
• 171559-74-3 tert-butyl 2-(3-nitro-2-oxopyridin-1(2H)-yl)acetate 
• 6332-56-5 2-hydroxy-3-nitropyridine 
• 105-36-2 ethyl bromoacetate 
• 147283-76-9 ethyl 3-nitro-2-oxo-1,2-dihydro-1-pyridylacetate 

Downstream Products

• 179524-57-3 t-butyl [3-nitro-2-oxo-4-(3-phenylpropyl)-1,2,3,4-tetrahydropyridyl]acetate 
• 147283-74-7 ethyl 3-amino-2-oxo-1,2-dihydro-1-pyridylacetate 

Relevant academic research and scientific papers

TRANSGLUTAMINASE 2 (TG2) INHIBITORS

Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.

Tissue transgutaminase pyridinone deriv. as inhibitor

Pyridinone derivatives (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. Pyridinone derivatives of formula (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. E1, E2 : -CO- or -SO 2; Rc : -NYY1a, -NH-CH 2-COOH, -NH-CH(CH 3)-COOH, -NH-CH (CH 2CH 2SCH 3)-COOH, -NH-CH(CH 2OH)-COOH, -NH-CH(CH 2SH)-COOH, -NH-CH(CH 2CONH 2)-COOH,-NH-CH(CH 2CH 2CONH 2)-COOH, [(1-carboxy-2-methyl-propyl)amino], [(1-carboxy-2-methyl-butyl)amino], [(1-carboxy-3-methyl-butyl)amino], [(1-carboxy-2-hydroxy-propyl)amino], [(1-benzyl-2-hydroxy-2-oxo-ethyl)amino], [[2-hydroxy-2-oxo-1-(p-tolylmethyl)ethyl]amino], [(1-carboxy-3-hydroxy-3-oxo-propyl)amino], [(1-carboxy-4-hydroxy-4-oxo-butyl)amino], piperazin-1-yl, morpholino, 1-piperidyl, (4-phenylpiperazin-1-yl), (4-benzylpiperazin-1-yl), (4-phenylpiperazin-1-yl), (4-methylpiperazin-1-yl), (2-oxo-1-piperidyl), (2,6-dioxo-1-piperidyl), isoindolin-2-yl, azepan-1-yl, azetidin-1-yl, aziridin-1-yl, 4,5-dihydrotriazol-1-yl, (3-methylimidazolidin-1-yl), pyrrolidin-1-yl, (2-oxopyrrolidin-1-yl), or (2,5-dioxopyrrolidin-1-yl); and Z : -CH 3, -C 2H 5, -C 3H 7, -CH(CH 3) 2,-C 4H 9, -C 6H 5, -CH 2-C 6H 5, -OCH 3, -OC 2H 5, -OC 3H 7, -OCH(CH 3) 2, -OC 4H 9, -OC 6H 5, -OCH 2C 6H 5, -OCH=CH 2 or -OCH 2-CH=CH 2. N.B. Rd is not defined. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a pharmaceutical composition comprising (I) and carrier, excipient or solvent; and (2) preparation of (I). [Image] ACTIVITY : Antiinflammatory; Neuroprotective; Anticonvulsant; Nootropic; Antiparkinsonian; Ophthalmological; Antiseborrheic; Dermatological; Antipsoriatic; Thrombolytic. MECHANISM OF ACTION : Transglutaminase 2 inhibitor.

Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives

Glycogen phosphorylase (GP) plays a crucial role in the conversion of glycogen to glucose-1-phosphate (and in turn glucose) and is a promising target for therapeutic intervention in diabetes. In this study we synthesized new derivatives of 2-oxo-1,2-dihyd

Aromatic heterocyclic derivatives as enzyme inhibitors

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Investigation of the regioselectivity of alkylation of 3-nitropyridin-2(1H)-ones

Alkylation of 3-nitropyridin-2(1H)-ones in the presence of bases affords N-alkylated products and sometimes O-alkylated products. The yields and relative amounts of N- and O-alkylated products depend substantially on the size of the substituent at the C(6

2-SUBSTITUTED 3-(4-AMIDINOPHENYL)PROPIONIC ACID DERIVATIVES

2-Substituted 3-(4-amidinophenyl)propionic acid derivatives of the formula STR1 in which A, Ar and B have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.

Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors

Human leukocyte elastase (HLE) is a serine protease produced by neutrophils that has been implicated in diseases such as amphysema and cystic fibrosis. An HLE inhibitor may have therapeutic value in these diseases. An active site model of HLE bound to a t