452056-81-4

Usage

Uses

Used in Medicinal Chemistry:
N-4-[2-(4-Fluorophenyl)-acetyl]-pyridin-2-yl-acetaMide is used as a key intermediate in the synthesis of pharmaceuticals for its ability to contribute to the development of novel drug candidates. Its structural features, including the pyridine ring and fluorophenyl group, offer opportunities for further chemical modifications to enhance the pharmacological properties of the resulting compounds.
Used in Drug Discovery:
In the field of drug discovery, N-4-[2-(4-Fluorophenyl)-acetyl]-pyridin-2-yl-acetaMide is employed as a starting material for the design and synthesis of new bioactive molecules. Its potential biological activities, which are yet to be fully explored, may lead to the identification of compounds with therapeutic potential in various disease areas.
Used in Chemical Research:
N-4-[2-(4-Fluorophenyl)-acetyl]-pyridin-2-yl-acetaMide is also used as a research tool in chemical research to study the reactivity and properties of acetamide derivatives. This helps in understanding the fundamental chemical behavior of such compounds and may contribute to the development of new synthetic methods and strategies.

Upstream product

• 108-24-7 acetic anhydride 
• 452056-79-0 N-{4-[2-cyano-2-(4-fluorophenyl)acetyl]pyridin-2-yl}acetamide 
• 549505-57-9 N-{4-[2-cyano-2-(4-fluoro-phenyl)-1-hydroxy-vinyl]-pyridin-2-yl}-acetamide 
• 5327-32-2 2-acetylamino-4-methylpyridine 
• 695-34-1 2-Amino-4-methylpyridine 
• 459-22-3 4-fluorophenylacetonitrile 
• 452056-80-3 1-(2-aminopyridin-4-yl)-2-(4-fluorophenyl)ethanone 

Downstream Products

• 908380-97-2 N-{4-[5-(4-fluoro-phenyl)-3-methyl-2-methylsulfinyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide 
• 452056-88-1 C₁₇H₁₅FN₄OS 
• 452056-83-6 N-{4-[5-(4-fluorophenyl)-1-oxy-3-methyl-3H-imidazol-4-yl]pyridin-2-yl}acetamide 
• 549505-58-0 N-{4-[4-(4-fluorophenyl)-1-methyl-2-methylsulfanyl-1H-imidazol-5-yl]pyridin-2-yl}-N-(1-phenylethyl)amine 
• 452056-98-3 4-[4-(4-fluorophenyl)-1-methyl-2-methylsulfanyl-1H-imidazol-5-yl]pyridin-2-ylamine 
• 452056-93-8 N-{4-[4-(4-fluorophenyl)-1-methyl-2-methylsulfanyl-1H-imidazol-5-yl]pyridin-2-yl}acetamide 

Relevant academic research and scientific papers

Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases

The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 (PDE4), and the potential benefits arising from the blockage of both inflammation-related enzymes were thoroughly investigated. The most promising compound, CBS-3595 (1), was successively evaluated in in vitro experiments as well as in ex vivo and in vivo preclinical studies after administration of 1 to rodents, dogs, and monkeys. The resulting data clearly indicated a potent suppression of tumor necrosis factor alpha release. For reconfirming the findings of the animal studies when administering 1 to healthy human volunteers, a phase I clinical trial was conducted. Apart from further information regarding the pharmacokinetic and pharmacodynamic characteristics of 1, it was demonstrated that dual inhibition of p38α MAPK and PDE4 is able to synergistically attenuate the excessive anti-inflammatory response.

Tri- and tetrasubstituted imidazoles as p38α mitogen-activated protein kinase inhibitors

The synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles as potent p38α mitogen-activated protein kinase inhibitors is described. The trisubstituted imidazole series was found to be more potent than the tetrasubstituted imidazole seri

Imidazole compounds having an antiinflammatory effect

The invention relates to 2-sulfinyl- or 2-sulfonyl-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3 and R4 have the meaning indicated in the description. The compounds of the i

2-SULFINYL- AND 2-SULFONYL-SUBSTITUTED IMIDAZOLE DERIVATIVES AND THEIR USE AS CYTOKINE INHIBITORS

The invention relates to 2-sulfinyl- or 2-sulfonyl-substituted imidazole derivatives of the formula (I) in which the radicals R1, R2, R3 and R4 have the meaning indicated in the description. The compounds of the

Tetrasubstituted imidazole inhibitors of cytokine release: Probing substituents in the N-1 position

We prepared novel 1,2,4,5-tetrasubstituted imidazole derivatives with high anti-inflammatory activity by using our previously described regiospecific synthesis. Systematic optimization of the imidazole N-1 substituent resulted in compound 9b that potently

Identification of regioisomers in a series of N-substituted pyridin-4-yl imidazole derivatives by regiospecific synthesis, GC/MS, and 1H NMR

The regiospecific synthesis of 2a (Scheme 3), a novel and potent pyridinyl imidazole inhibitor of p38 MAP (mitogen-activated protein) kinase, and the regioselective preparation of its regioisomer 2b (Scheme 4) are described. Chromatographic and spectroscopic data are presented, which in this class of compounds allow the unambiguous identification of regioisomers prepared by a nonregiospecific synthetic strategy. Biological data demonstrating the importance of the correct regiochemistry for inhibition of p38 are given.