250683-77-3

Upstream product

• 109-01-3 1-methyl-piperazine 
• 250683-76-2 3-fluoro-4-(4-methylpiperazin-1-yl)benzoic acid 
• 64248-62-0 3,4-Difluorobenzonitrile 

Downstream Products

• 951906-87-9 (3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)methylamine 

Relevant academic research and scientific papers

Synthesis and evaluation of cyclic secondary amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents

In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, secondary amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.

Benzamide derivatives for the treatment of diseases mediated by cytokines

The invention concerns amide derivatives of Formula (I) wherein: R1and R2include hydroxy, C1-6alkoxy, mercapto, C1-6akylthio, amino and heterocyclyl; m and p are independently 0-3; R3is halo, cyano or C1-6alkoxy; q is 0-4; and R4is aryl or cycloalkyl wherein R4is optionally substituted with up to 3 substituents having any value defined for each R1group; or a pharmaceutically-acceptable salt or in-vivo-cleavable ester thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.