56205-88-0

Usage

Uses

Used in Pharmaceutical Industry:
4-(METHANESULFONYLAMINO)PHENYLACETIC ACID is used as a reagent for the preparation of resiniferatoxin analogs, which are metabolically stable TRPV1 agonists and potential analgesics. Its ability to form stable bonds with other molecules makes it an essential component in the synthesis of these pain-relieving agents.
Additionally, 4-(METHANESULFONYLAMINO)PHENYLACETIC ACID is used in the preparation and structure-activity relationships of 2,6-diaryl-4-(phenacylamino)pyrimidines, which are selective adenosine A2A antagonists. These compounds have potential applications in the treatment of various diseases, including neurodegenerative disorders and cancer, by modulating adenosine receptor signaling pathways.

InChI:InChI=1/C9H11NO4S/c1-15(13,14)10-8-4-2-7(3-5-8)6-9(11)12/h2-5,10H,6H2,1H3,(H,11,12)

Upstream product

• 1197-55-3 4-aminophenylacetic acid 
• 124-63-0 methanesulfonyl chloride 
• 58827-89-7 ethyl 4-(N-methylsulfonylamino)phenylacetate 
• 5438-70-0 ethyl (4-amino-3,5-dibromophenyl)acetate 

Downstream Products

• 401573-59-9 pentafluorophenyl 2-[4-(methylsulfonylamino)phenyl]acetate 
• 1015484-09-9 C₂₃H₂₄N₆O₄S 
• 1134165-16-4 C₃₇H₄₂N₂O₈S 
• 1134164-95-6 C₃₇H₄₁NO₉S 

Relevant academic research and scientific papers

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts

A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity (50 nM) together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay. Mechanistic studies through resistance selection with one of the analogues followed by whole-genome sequencing implicated the P. falciparum cyclic amine resistance locus in the mode of resistance.

COMPOUNDS AND THEIR METHODS OF USE

Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES AS GLUTAMINASE INHIBITORS FOR TREATING CANCERS THEREOF

Provided are compounds of formula (I), wherein X, Y, Z, W, m, n, o, p, R1, R2 and R6 are defined as in the description. Pharmaceutical compositions and uses as glutaminase inhibitors for treating cancers thereof are also provided.

COMPOUNDS AND THEIR METHODS OF USE

Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.

Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity

Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.

Sulfonylamino phenylacetamide derivatives and methods of their use

Sulfonylamino phenylacetamide derivatives of the general formula are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed. In certain embodiments, the compounds of the invention that, preferably: (1) bind with high affinity to κ opioid receptors; (2) display good opioid receptor selectivity of κ versus μ and κ versus δ; and (3) do not substantially inhibit cytochrome P450 enzymatic activity, in particular CYP2D6, CYP2C9 and CYP3A4.

NOVEL N-HYDROXY THIOUREA, UREA AND AMIDE COMPOUNDS AND THE PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention relates to novel n-hydroxythiourea, urea and amide compounds as a potent vanilloid receptor antagonist and the pharmaceutical compositions comprising the same. The inventive compound can be useful for analgesics to prevent, alleviate

Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: Discovery of an N-hydroxythiourea analogue with potent analgesic activi

The structural modifications on the B-region of the potent and high affinity vanilloid receptor (VR1) lead ligand N-(3-acyloxy-2-benzylpropyl)- N′-[4-(methylsulfonylamino)benzyl]thiourea were investigated by the replacement of the thiourea with

Antiarrhythmic compounds

The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) whereinR1 /