88327-91-7

Usage

Uses

Used in Organic Synthesis:
4-(PYRROLIDINE-1-SULFONYL)-PHENYLAMINE is used as a synthetic intermediate for the creation of more complex organic molecules. Its unique structure, combining phenylamine and pyrrolidine components, provides versatility in chemical reactions, facilitating the development of new compounds with potential applications in various industries.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, 4-(PYRROLIDINE-1-SULFONYL)-PHENYLAMINE is used as a building block for the development of new drugs. Its semisynthetic amino acid derivative nature allows for the design of peptide-based therapeutics, potentially targeting specific biological pathways or diseases.
Used in Chemical Research:
4-(PYRROLIDINE-1-SULFONYL)-PHENYLAMINE serves as a subject of study in chemical research, where its properties and reactivity are explored. Understanding its behavior in various chemical reactions can lead to the discovery of new synthetic routes or applications in different fields.
While the exact uses and applications of 4-(PYRROLIDINE-1-SULFONYL)-PHENYLAMINE may not be widely reported, its role in organic synthesis, pharmaceutical development, and chemical research highlights its potential value in creating new compounds and advancing scientific knowledge.

InChI:InChI=1/C10H14N2O2S/c11-9-3-5-10(6-4-9)15(13,14)12-7-1-2-8-12/h3-6H,1-2,7-8,11H2

Upstream product

• 175278-37-2 1-((4-nitrophenyl)sulfonyl)pyrrolidine 
• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 121-60-8 p-acetylaminobenzenesulfonyl chloride 

Downstream Products

• 94243-29-5 [4-(Pyrrolidine-1-sulfonyl)-phenylamino]-acetonitrile 
• 88327-96-2 2-((4-(pyrrolidin-1-ylsulfonyl)phenyl)amino)acetic acid 
• 327067-60-7 C₁₇H₁₇FN₂O₃S 
• 349627-22-1 C₁₅H₁₆N₂O₄S 
• 327067-64-1 C₁₅H₁₆N₂O₃S₂ 
• 88328-02-3 C₁₂H₁₅N₃O₅S 
• 88323-70-0 1-[4-(Pyrrolidine-1-sulfonyl)-phenyl]-1H-pyrazole-3,4-dicarboxylic acid dimethyl ester 

Relevant academic research and scientific papers

Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors

We report on the discovery of norbornyl moiety as a novel structural motif for cyclin-dependent kinase 2 (CDK2) inhibitors which was identified by screening a carbocyclic nucleoside analogue library. Three micromolar hits were expanded by the use of medic

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors

The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57-617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and reassay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.

1,2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors

A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50 = 1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.

Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease

Tissue transglutaminase 2 (TG2) is a multifunctional protein primarily known for its calcium-dependent enzymatic protein cross-linking activity via isopeptide bond formation between glutamine and lysine residues. TG2 overexpression and activity have been found to be associated with Huntington's disease (HD); specifically, TG2 is up-regulated in the brains of HD patients and in animal models of the disease. Interestingly, genetic deletion of TG2 in two different HD mouse models, R6/1 and R6/2, results in improved phenotypes including a reduction in neuronal death and prolonged survival. Starting with phenylacrylamide screening hit 7d, we describe the SAR of this series leading to potent and selective TG2 inhibitors. The suitability of the compounds as in vitro tools to elucidate the biology of TG2 was demonstrated through mode of inhibition studies, characterization of druglike properties, and inhibition profiles in a cell lysate assay.

4,6-DIAMINONICOTINAMIDE COMPOUND

[Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction. [Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu4 positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu4 PAM reported to date.

Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex

Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds could conceivably diminish these statistics and pr

Pyrazolo [1,5-A] pyrimidine adenosine A2a receptor antagonists

Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

NOVEL ADENOSINE A3 RECEPTOR AGONISTS

The invention realizes that a series of sulfonamido derivatives with a conserved uronamide group at the 5' position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido deritatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.

Neuropeptide Y antagonists

The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.