74418-15-8

Usage

Uses

Used in Pharmaceutical Research:
1-(3-Trifluoromethylphenyl)-[1,4]diazepane is used as a potential drug candidate in pharmaceutical research for its potential therapeutic effects. 1-(3-Trifluoromethylphenyl)-[1,4]diazepane's unique structure and properties make it a promising candidate for treating a variety of medical conditions or diseases.
Used in Medicinal Chemistry:
In the field of medicinal chemistry, 1-(3-Trifluoromethylphenyl)-[1,4]diazepane is employed for its potential to contribute to the development of new drugs and therapies. Its specific chemical features and properties may offer advantages in the design and synthesis of novel pharmaceutical agents.

InChI:InChI=1/C12H15F3N2/c13-12(14,15)10-3-1-4-11(9-10)17-7-2-5-16-6-8-17/h1,3-4,9,16H,2,5-8H2

Upstream product

• 147378-75-4 1-(3-Trifluoromethylphenyl)hexahydro-1,4-diazepin-5-one 
• 401-81-0 m-trifluoromethylphenyl iodide 
• 112275-50-0 tert-butyl 1,4-diazepine-1-carboxylate 

Downstream Products

• 193611-12-0 C₁₅H₂₀ClF₃N₂ 

Relevant academic research and scientific papers

Structure-activity relationship of sulfonyl piperazine LpxH inhibitors analyzed by an LpxE-coupled malachite green assay

The UDP-2,3-diacylglucosamine pyrophosphatase LpxH in the Raetz pathway of lipid A biosynthesis is an essential enzyme in the vast majority of Gram-negative pathogens and an excellent novel antibiotic target. The 32P-radioautographic thin-layer chromatography assay has been widely used for analysis of LpxH activity, but it is inconvenient for evaluation of a large number of LpxH inhibitors over an extended time period. Here, we report a coupled, nonradioactive LpxH assay that utilizes the recently discovered Aquifex aeolicus lipid A 1-phosphatase LpxE for quantitative removal of the 1-phosphate from lipid X, the product of the LpxH catalysis; the released inorganic phosphate is subsequently quantified by the colorimetric malachite green assay, allowing the monitoring of the LpxH catalysis. Using such a coupled enzymatic assay, we report the biochemical characterization of a series of sulfonyl piperazine LpxH inhibitors. Our analysis establishes a preliminary structure-activity relationship for this class of compounds and reveals a pharmacophore of two aromatic rings, two hydrophobic groups, and one hydrogen-bond acceptor. We expect that our findings will facilitate the development of more effective LpxH inhibitors as potential antibacterial agents.

4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)- N -(4-methoxypyridin-2-yl) piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth

4′-Phosphopantetheinyl transferases (PPTases) catalyze a post-translational modification essential to bacterial cell viability and virulence. We present the discovery and medicinal chemistry optimization of 2-pyridinyl-N-(4-aryl)piperazine-1-carbothioamides, which exhibit submicromolar inhibition of bacterial Sfp-PPTase with no activity toward the human orthologue. Moreover, compounds within this class possess antibacterial activity in the absence of a rapid cytotoxic response in human cells. An advanced analogue of this series, ML267 (55), was found to attenuate production of an Sfp-PPTase-dependent metabolite when applied to Bacillus subtilis at sublethal doses. Additional testing revealed antibacterial activity against methicillin-resistant Staphylococcus aureus, and chemical genetic studies implicated efflux as a mechanism for resistance in Escherichia coli. Additionally, we highlight the in vitro absorption, distribution, metabolism, and excretion and in vivo pharmacokinetic profiles of compound 55 to further demonstrate the potential utility of this small-molecule inhibitor.

THIENOPYRIDINE DERIVATIVES

The present invention provides a compound promoting osteogenesis. The present invention provides a compound having the following general formula (I) wherein R 1 is H or alkyl, R 2 is R a S-, R a O-, R a NH-, R a (R b )N- or cyclic amino, and R a and R b are alkyl which may be substituted, cycloalkyl which may be substituted, or the like, or a pharmacologically acceptable salt thereof.

Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists

Pharmacologically active benzimidazolone derivatives as 5-HT1Aand 5-HT2 receptors, useful in the treatment of CNS disorders of formula: wherein, R1 and R2 may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C1 6 alkyl, C1 6 alkoxy, C1 6 alkylthio, C1 6 acyl, carboxyl, C1 6 alkoxy- carbonyl, hydroxy, nitro, amino optionally C1 4 alkyl N-mono or di-substituted, C1 6 acylamino, C1 6 alkoxycarbonylamino, carbamoyl optionally C1 4 alkyl N-mono or di-substituted, cyano, C1 6 alkylsulphinyl, C1 6 alkylsulphonyl, amino sulphonyl optionally C1 4 alkyl N-mono or di-substituted, C1 4 alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino;, R3 is hydrogen, C1 6 alkyl, C2 6 alkenyl or C2-C6 alkynyl;, A is -CO- or -CONH- or it is absent;, B is a straight or branched, saturated or unsaturated C2 6 alkyl;, m and n are both independently an integer from 1 to 3;, R4 is an aryl, aralkyl, a heteroaryl or heteroaralkyl group, each group being optionally substituted by one or more substituents selected from halogen, trifluoromethyl, cyano, C1 3 alkoxy, C1 4 alkyland acid addition salts thereof., The process for the preparation of the compounds of formula I as well as pharmaceutical compositions containing them are also described.