173951-83-2

Upstream product

• 98-74-8 4-Nitrobenzenesulfonyl chloride 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 

Downstream Products

• 1306720-92-2 N-[4-(4-ethyl-piperazine-1-sulfonyl)-phenyl]-acrylamide 
• 1306720-97-7 N-{4-[4-(3-pyridin-3-yl-propionyl)-piperazine-1-sulfonyl]-phenyl}-acrylamide 
• 1306720-05-7 N-[4-(4-benzoyl-piperazine-1-sulfonyl)-phenyl]-acrylamide 
• 1306721-26-5 4-[4-(acryloyl-methyl-amino)-benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1306722-72-4 4-(4-(but-2-enoylamino)benzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1306720-00-2 4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1306720-49-9 N-{4-[4-(piperidine-1-carbonyl)piperazine-1-sulfonyl]phenyl}acrylamide 
• 1306721-50-5 N-{4-[4-(octahydroisoquinoline-2-carbonyl)piperazine-1-sulfonyl]phenyl}acrylamide 
• 1306720-47-7 4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid cyclopentyl ester 
• 1306720-33-1 4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid ethyl ester 
• 1306720-35-3 4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid methyl ester 
• 1357382-24-1 N-(4-{4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl}-phenyl)acrylamide 
• 1306721-04-9 N-(4-{4-[2-(3-phenoxyphenyl)acetyl]piperazine-1-sulfonyl}-phenyl)acrylamide 
• 1306720-18-2 4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-2-ylmethyl ester 

Relevant academic research and scientific papers

Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer's disease

Based on our previous work, a series of N-phenyl-3-methoxy-4-pyridinone derivatives were designed as orally bioavailable dual functional agents for therapy of Alzheimer's disease, through introducing alkyloxy moiety into 4-pyridinone ring to avoid the pos

1,4-naphthoquinone derivative, preparation method and applications thereof

The invention relates to a 1,4-naphthoquinone derivative, a preparation method and applications thereof. According to the present invention, the 1,4-naphthoquinone derivative is firstly synthesized, has good activity in the inhibition of human colon cance

HEPATITIS B VIRAL ASSEMBLY EFFECTORS

Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.

Discovery of sulfonamidebenzamides as selective apoptotic CHOP pathway activators of the unfolded protein response

Cellular proteins that fail to fold properly result in inactive or disfunctional proteins that can have toxic functions. The unfolded protein response (UPR) is a two-tiered cellular mechanism initiated by eukaryotic cells that have accumulated misfolded p

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.

Irreversible 4-aminopiperidine transglutaminase 2 inhibitors for Huntington's disease

A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure-activity relationship of this new series and report on the transglutaminase selectivity and in vitro ADME properties of selected compounds. We demonstrate that the compounds do not conjugate glutathione in an in vitro setting and have superior plasma stability over our previous series.

TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.

Antiplasmodial activity of piperazine sulfonamides

A high-throughput screening program identified two piperazine sulfonamides with activity against Plasmodium falciparum. Both screening positives had three structural features with potential liabilities: furanyl, thiourea and nitrophenyl groups. The furan could be replaced with no loss of activity, replacement of the nitrophenyl led to some loss of activity, and any attempt to replace the thiourea led to a significant decrease in activity, which implicates this reactive functional group's role in the antiplasmodial activity of this compound class.

THIAZOLE INHIBITORS TARGETING RESISTANT AND KINASE MUTATIONS

A compound is provided, having the general structure (A): wherein A is an aryl or heteroaryl group, Y is a hydrophobic linking moiety, and L is a substitutent. The compound (A) can be used for treatment of various angiogenic-associated or hematologic disorders, such as myeloproliferative disorders in patients who do not respond to kinase-inhibition therapy that comprises administering currently used medications.

Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.