66000-40-6

Usage

Biological Activity

bw 755c is a dual inhibitor of 5-lipoxygenase (5-lo) and cyclooxygenase (cox) pathways.constitutive cyclooxygenase (cox-1) is present in cells under physiological conditions, whereas cox-2 is induced by some cytokines, mitogens, and endotoxin in pathological conditions, such as inflammation. since 5-lipoxygenase (5-lo) oxidizes arachidonic acid to 5-hydroperoxyeicosatetraenoic acid in the first step of the leukotriene pathway, 5-lo inhibitors should prevent leukotriene biosynthesis and thus prove useful in the treatment of allergic asthma.

in vitro

previous study found that bw 755c and other nonsteroidal antiinflammatory drugs including diclofenac, acetaminophen, and naproxen showed approximately equipotent inhibitory effects on cox-1 and cox-2 in intact cells. whereas, bf 389 was the most potent and most selective inhibitor of cox-2 in intact cells [1].

in vivo

an animal study was conducted to examine whether bw-755c delayed neuronal death in the hippocampal ca1 sector in mongolian gerbils after 5 minutes of forebrain ischemia. gerbils were injected with bw-755c. seven days after ischemic insult, the animals were perfusion-fixed, and the neuronal density in the hippocampal ca, sector was estimated. results showed that in ischemic gerbils with vehicle administration, the average neuronal density was 13 for bw-755c. in ischemic gerbils treated with 30 mg/kg bw-755c, the average neuronal densities was 14 [2].

IC 50

0.75 μm, 0.65 μg/ml, and 1.2 μg/ml for 5-lo, cox-1, and cox-2, respectively

references

[1] mitchell, j. a.,akarasereenont, p.,thiemermann, c., et al. selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. proceedings of the national academy of sciences of the united states of america 90, 11693-11697 (1993). [2] nakagomi t, sasaki t, kirino t, tamura a, noguchi m, saito i, takakura k. effect of cyclooxygenase and lipoxygenase inhibitors on delayed neuronal death in the gerbil hippocampus. stroke. 1989 jul;20(7):925-9.

InChI:InChI=1/C10H10F3N3/c11-10(12,13)7-2-1-3-8(6-7)16-5-4-9(14)15-16/h1-3,6H,4-5H2,(H2,14,15)

Upstream product

• 107-13-1 acrylonitrile 
• 368-78-5 3-(trifluoromethyl)phenylhydrazine 
• 3107-33-3 3-(trifluoromethyl)phenylhydrazine hydrochloride 
• 126583-33-3 β-(3-trifluoromethylphenylamino)-propionamidoxime*HCl 
• 126583-34-4 5-(4-chlorophenyl)-3-<2-(3-trifluoromethylphenyl)-aminoethyl>-1,2,4-oxadiazole 
• 126646-34-2 4,5-dihydro-3-(4-chlobenzoylamino)-1-(3-trifluoromethylphenyl)-1H-pyrazole 

Downstream Products

• 126583-26-4 4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1H-pyrazol 
• 126583-25-3 3-(2,5-Dimethyl-pyrrol-1-yl)-1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1H-pyrazole 
• 77992-48-4 N-[1-(3-Trifluoromethyl-phenyl)-4,5-dihydro-1H-pyrazol-3-yl]-acetamide 
• 162999-58-8 N,N-Dimethyl-N'-[1-(3-trifluoromethyl-phenyl)-4,5-dihydro-1H-pyrazol-3-yl]-formamidine 
• 66000-41-7 1-(3-(trifluoromethyl)phenyl)-3-amino-1H-pyrazole 
• 95883-77-5 1-(3-Trifluoromethylphenyl)-4,5-dihydro-N-(4-methoxy phenyl)-1H-pyrazol-3-amine 
• 83672-09-7 3-(2-4'-carboxybutoxy-6-hydroxybenzylideneamino)-1-(3-trifluoromethylphenyl)-2-pyrazoline 
• 83908-35-4 3-Propionamido-1-(3-trifluoromethylphenyl)-2-pyrazoline 
• 83908-80-9 3-isobutyramido-1-(3-trifluoromethylphenyl)-2-pyrazoline 

Relevant academic research and scientific papers

PYRIDO[3,4-D]PYRIMIDINYL ACETAMIDE DERIVATIVES AS TRPA1 MODULATORS

Provided are pyrido[3,4-d]pyrimidinyl acetamide derivatives as Transient Receptor Potential Ankyrin (TRPA) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Transient Receptor Potential Ankyrin 1 (TRPAl). Also provided herein are processes for preparing the compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1. Formula (I).

2-(benzimidazol-1-yl)-acetamide bisaryl derivatives

The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

Phenol compound having antioxidative activity and the process for preparing the same

Disclosed are a phenol compound represented by the formula (1): STR1 wherein R0 represents H, alkyl or alkyloxy; R1 represents alkyl; R2 represents alkyl or alkyloxy; OR3 represents OH; R4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR7 ; where R7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): STR2 represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom, or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

3-Trifluoroacetylamino-1-aryl-2-pyrazolines

This disclosure describes novel 3-substituted amino-1-phenyl-2-pyrazolines and 3-substituted amino-1-mono and disubstituted phenyl-2-pyrazolines and their C4 and C5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.