28093-57-4

Upstream product

• 536-90-3 m-Anisidine 
• 1493-27-2 ortho-nitrofluorobenzene 
• 104-94-9 4-methoxy-aniline 
• 2398-37-0 3-methoxyphenyl bromide 
• 88-74-4 2-nitro-aniline 
• 88-73-3 2-Chloronitrobenzene 

Downstream Products

• 1033224-86-0 N-(3-methoxyphenyl)benzene-1,2-diamine 

Relevant academic research and scientific papers

A rhodamine-based fast and selective fluorescent probe for monitoring exogenous and endogenous nitric oxide in live cells

Nitric oxide, an important cellular messenger molecule, plays a wide range of physiological roles in neurotransmission, vascular relaxation, platelet activation, and immune response. In this work, we synthesized a selective and sensitive cationic fluorescent probe (ROPD) for monitoring exogenous and endogenous nitric oxide in live cells by grafting a NO-trapper o-phenylenediamine (OPD), via one of the amino groups of OPD, onto a rhodamine fluorophore at the C-3 position. The probe exhibited high selectivity and sensitivity towards NO with fast response in the water phase over a wide pH range. At the same time, the probe ROPD is cell-membrane permeable and can be used for the real-time visualization of exogenous NO in both L929 and HeLa cells, and endogenous NO in stressed RAW 264.7 cells.

Design, synthesis and antifungal evaluation of novel pyrazole carboxamides with diarylamines scaffold as potent succinate dehydrogenase inhibitors

Sixteen novel pyrazole carboxamides with diarylamines scaffold were designed, synthesized and characterized in detail via 1H NMR, 13C NMR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good ant

Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-Aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3 H)-yl]-1-(methylamino)butan-2- ols (WYE-103231)

Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol- 1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound S-17b (WYE-103231) had low nanomolar hNET potency (IC50 = 1.2 nM) and excellent selectivity for hNET over hSERT (>1600-fold) and hDAT (>600-fold). S-17b additionally had a good pharmacokinetic profile and demonstrated oral efficacy in rat models of ovariectomized-induced thermoregulatory dysfunction and morphine dependent flush as well as the hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain.

4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Potent and selective p70S6 kinase inhibitors

We report herein the design and synthesis of 4-(benzimidazol-2-yl)-1,2,5-oxadiazol-3-amine derivatives as inhibitors of p70S6 kinase. Screening hits containing the 4-(benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine scaffold were optimized for p70S6K potency and selectivity against related kinases. Structure-based design employing an active site homology model derived from PKA led to the preparation of benzimidazole 5-substituted compounds 26 and 27 as highly potent inhibitors (Ki 100-fold selectivity against PKA, ROCK and GSK3.

ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE

The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Efficient methods for the synthesis of 2-hydroxyphenazine based on the Pd-catalyzed N-arylation of aryl bromides

(Chemical Equation Presented) Substituted diphenylamines can be synthesized by Pd(0)-catalyzed N-arylation using o-nitroanilines and nitro-substituted aryl bromides for a substrate. Cyclization of the diphenylamines by various methods, including the intramolecular Pd(0)-catalyzed N-arylation, produces 2-methoxyphenazine which can easily be deprotected to give 2-hydroxyphenazine. This phenazine is required to synthesize methanophenazine, a novel redoxactive cofactor isolated from methanogenic archaea.

New Modified Preparation of 2-Nitrodiarylamines

2-Nitrodiarylamines are prepared in good yields from 2-chloronitrobenzene and anilines in the presence of potassium fluoride without solvent at 160-170 deg C.